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Lee C Mangum, Xiang Hou, Abdolsamad Borazjani, Jung Hwa Lee, Matthew K Ross, J Allen Crow
Macrophage foam cells store excess cholesterol as cholesteryl esters, which need to be hydrolyzed for cholesterol efflux. We recently reported that silencing expression of carboxylesterase 1 (CES1) in human THP-1 macrophages (CES1KD macrophages) reduced cholesterol uptake and decreased expression of CD36 and scavenger receptor-A in cells loaded with acetylated low-density lipoprotein (acLDL). Here, we report that CES1KD macrophages exhibit reduced transcription of cytochrome P450 27A1 ( CYP27A1 ) in non-loaded and acLDL-loaded cells...
January 10, 2018: Biochemical Journal
Yi Zhang, Jing Li, Zhuo Ma, Chao Shan, Xiwu Gao
Two unique housefly strains, MSS and N-MRS, were selected and used to clarify mechanisms of sex-associated malathion resistance in the housefly, Musca domestica. Compared with the lab-susceptible CSS strain, susceptible females and resistant males were observed in the malathion-susceptible MSS strain, while the malathion-resistant near-isogenic line, N-MRS, achieved similar resistance level between genders. Significant synergistic effect of the esterase-inhibitor DEF on resistant houseflies pointed to the important involvement of esterase in this specific malathion resistance...
January 9, 2018: Scientific Reports
Shenggan Wu, Xinfang Li, Xinju Liu, Guiling Yang, Xuehua An, Qiang Wang, Yanhua Wang
Pesticide contamination is more often found as a mixture of different pesticides in water bodies rather than individual compounds. However, regulatory risk evaluation is mostly based on the effects of individual pesticides. In the present study, we aimed to investigate the individual and joint toxicities of triazophos (TRI) and imidacloprid (IMI) to the zebrafish (Danio rerio) using acute indices and various sublethal endpoints. Results from 96-h semi-static test indicated that the LC50 values of TRI to D. rerio at multiple life stages (embryonic, larval, juvenile and adult stages) ranged from 0...
January 6, 2018: Environmental Pollution
Yuuta Fujikawa, Taiki Nampo, Masaya Mori, Manami Kikkawa, Hideshi Inoue
Pi class glutathione S-transferase (GSTP1) is highly expressed in various cancerous cells and pre-neoplastic legions, where it is involved in apoptotic resistance or metabolism of several anti-tumour chemotherapeutics. Therefore, GSTP1 is a marker of malignant and pre-malignant cells and is a promising target for visualization and drug development. Here we demonstrate that fluorescein diacetate (FDA), a fluorescent probe used for vital staining, is a fluorescently activated by esterolytic activity of human GSTP1 (hGSTP1) selectively among various cytosolic GSTs...
March 1, 2018: Talanta
Yiji Li, Jiabao Xu, Daibin Zhong, Hong Zhang, Wenqiang Yang, Guofa Zhou, Xinghua Su, Yang Wu, Kun Wu, Songwu Cai, Guiyun Yan, Xiao-Guang Chen
BACKGROUND: Aedes albopictus (Skuse) is an invasive mosquito that has become an important vector of chikungunya, dengue and Zika viruses. In the absence of specific antiviral therapy or a vaccine, vector management is the sole method available for reducing Aedes-induced disease morbidity. Determining the resistance status of Ae. albopictus to insecticides and exploring the resistance mechanisms is essential for future vector control planning. METHODS: Aedes albopictus larvae and pupae were sampled from six sites (two sites each from urban, suburban and rural) in Guangzhou...
January 3, 2018: Parasites & Vectors
Amira Abdel-Daim, Kayoko Ohura, Teruko Imai
In the present study, we established a quantitative western blotting method to measure the expression level of recombinant serine hydrolases based on their catalytic mechanism. Fluorophosphonate (FP) biotin was selected as a universal probe to quantify their expression level, since FP moiety irreversibly inhibits serine hydrolases through strong stoichiometric binding to active serine residue. The linearity of detection using FP-biotin was assessed on three serine hydrolases; human carboxylesterase (CES) 1, butyrylcholinesterase and porcine liver esterases (PLE)...
December 28, 2017: European Journal of Pharmaceutical Sciences
Valerio De Vitis, Cristina Nakhnoukh, Andrea Pinto, Martina Letizia Contente, Alberto Barbiroli, Mario Milani, Martino Bolognesi, Francesco Molinari, Louise J Gourlay, Diego Romano
Microbial carboxylesterases are important biocatalysts that selectively hydrolyze an extensive range of esters. Here, we report the biochemical and structural characterization of an atypical carboxylesterase from Bacillus coagulans (BCE), endowed with high enantioselectivity towards different 1,2-O-isopropylideneglycerol (IPG or solketal) esters. BCE efficiently catalyzes the production of enantiopure (S)-IPG, a chiral building block for the synthesis of β-blockers, glycerophospholipids and prostaglandins; efficient hydrolysis was observed up to 65°C...
December 26, 2017: FEBS Journal
Chen Shaojun, Hua Li, Huang Haixin, Li Guisheng
Topoisomerase 1 (TOPO-1) and carboxylesterase 2 (CES-2) are found to play crucial roles in the pathogenesis of various cancers. The prognostic role of TOPO-1 and CES-2 in patients with metastatic colorectal cancer (mCRC) who underwent irinotecan chemotherapy was largely unknown. In the current study, we assessed the expression of TOPO-1 and CES-2 in mCRC and analyzed its potential relevance to irinotecan based therapy. A total of 98 patients with mCRC were included in this study. The expression of TOPO-1 and CES-2 in mCRC tissues was evaluated by immunohistochemistry...
December 20, 2017: Cancer Biology & Therapy
Jiesi Xu, Yang Xu, Yanyong Xu, Liya Yin, Yanqiao Zhang
Atherosclerotic cardiovascular disease is a leading cause of death in the western world. Increased plasma triglyceride and cholesterol levels are major risk factors for this disease. Carboxylesterase 1 (Ces1/Ces1g) has been shown to play a role in metabolic control. So far, the role of mouse Ces1/Ces1g deficiency in atherosclerosis is not elucidated. We generated Ces1/Ces1g -/- mice. Compared to wild-type mice, Ces1/Ces1g -/- mice had reduced plasma cholesterol levels. We then generated Ces1g -/- Ldlr -/- double knockout (DKO) mice, which were fed a Western diet for 16 weeks...
December 19, 2017: Scientific Reports
Ayan Srivastava, Ashwini Kumar Nigam, Swati Mittal, Ajay Kumar Mittal
Enhancement of immune system seems to be the most promising method of preventing fish diseases. Several herbal products have immunostimulant properties, and are environmental friendly, economical and can act against a broad spectrum of pathogens. Present study was designed with an aim to evaluate the role of aloin, extracted from a herb Aloe barbadensis, in the modulation of certain immune parameters in an Indian major carp, Labeo rohita. Fishes were divided into control, vehicle control and aloin treated groups...
December 11, 2017: Fish & Shellfish Immunology
Jin-Zi Ji, Bei-Bei Huang, Tong-Tong Gu, Ting Tai, Huan Zhou, Yu-Meng Jia, Qiong-Yu Mi, Meng-Ran Zhang, Hong-Guang Xie
Clopidogrel is predominantly hydrolyzed to clopidogrel carboxylic acid (CCA) by carboxylesterase 1, and subsequently CCA is glucuronidated to clopidogrel aryl glucuronide (CAG) by uridine diphosphate-glucuronosyltransferases (UGTs); however, the UGT isoenzymes glucuronidating CCA remain unidentified to date. In this study, the glucuronidation of CCA was screened with pooled human liver microsomes (HLMs) and 7 human recombinant UGT (rUGT) isoforms. Results indicated that rUGT2B7 exhibited the highest catalytical activity for the CCA glucuronidation as measured with a mean Vmax value of 120...
December 14, 2017: Biopharmaceutics & Drug Disposition
Laurent Salade, Nathalie Wauthoz, Magali Deleu, Marjorie Vermeersch, Carine De Vriese, Karim Amighi, Jonathan Goole
The aim of the present study was to develop a ghrelin-containing formulation based on liposomes coated with chitosan intended for nose-brain delivery for the treatment of cachexia. Among the three types of liposomes developed, anionic liposomes provided the best results in terms of encapsulation efficiency (56%) and enzymatic protection against trypsin (20.6% vs 0% for ghrelin alone) and carboxylesterase (81.6% vs 17.2% for ghrelin alone). Ghrelin presented both electrostatic and hydrophobic interactions with the anionic lipid bilayer, as demonstrated by isothermal titration calorimetry...
2017: International Journal of Nanomedicine
Zhuo Ma, Jing Li, Yi Zhang, Chao Shan, Xiwu Gao
Imidacloprid is a neonicotinoid insecticide that is effective against house fly, Musca domestica L., which is a major pest with the ability to develop resistance to insecticides. In the present study, we investigated the inheritance mode, the cross-resistance pattern and the mechanisms of resistance to imidacloprid. A near-isogenic house fly line (N-IRS) with 78-fold resistance to imidacloprid was used to demonstrate the mode of inheritance. The overlapping confidence limits of LC50 values and the slopes of the log concentration-probit lines between the reciprocal F1 and F1' progenies suggest that imidacloprid resistance is inherited autosomally in the house fly...
2017: PloS One
Li-Wei Zou, Qiang Jin, Dan-Dan Wang, Qing-Kai Qian, Da-Cheng Hao, Guang-Bo Ge, Ling Yang
Mammalian carboxylesterases are key serine hydrolases that catalyze the hydrolysis of a wide variety of ester compounds into the corresponding carboxylic acids and alcohols. In human, two major carboxylesterases, CES1 and CES2, have been identified and well-studied over the past decade. CES1 inhibitors have potential applications in the treatment of hypertriglyceridaemia, obesity and type 2 diabetes, owing to that this enzyme plays prominent role in the metabolism of cholesteryl esters. CES2 plays crucial roles in the metabolic activation of many prodrugs including anticancer agents capecitabine and CPT-11...
December 4, 2017: Current Medicinal Chemistry
Jinfang Jiang, Xiaoyan Chen, Dafang Zhong
Vicagrel, a structural analog of clopidogrel, is now being developed as a thienopyridine antiplatelet agent in a phase II clinical trial in China. Some studies have shown that vicagrel undergoes complete first-pass metabolism in human intestine, generating the hydrolytic metabolite 2-oxo-clopidogrel via carboxylesterase-2 (CES2) and subsequently the active metabolite H4 via CYP450s. This study aimed to identify hydrolases other than CES2 that are involved in the bioactivation of vicagrel in human intestine...
2017: Frontiers in Pharmacology
Kyeongnam Kim, Hwang-Ju Jeon, Sung-Deuk Choi, Daniel C W Tsang, Patryk Oleszczuk, Yong Sik Ok, Hoi-Seon Lee, Sung-Eun Lee
Individual and combined toxicities of endosulfan (ENDO) with phenanthrene (PHE) were evaluated using zebrafish (Danio rerio) adults. The 96-h LC50 values for ENDO and PHE were 4.6 μg L-1 and 920 μg L-1, respectively. To evaluate the mixture toxicity, LC10 and LC50 concentrations were grouped into four combinations as ENDO-LC10 + PHE-LC10, ENDO-LC10 + PHE-LC50, ENDO-LC50 + PHE-LC10, and ENDO-LC50 + PHE-LC50, and their acute toxicities were determined. The combination of LC50-ENDO and LC10-PHE exhibited a synergistic effect...
November 23, 2017: Chemosphere
Ülkü Akyol Ardıç, Eyüp Sabri Ercan, Duygu Aygüneş, Deniz Yüce, Sibel Durak, Buket Kosova
OBJECTIVE: Methylphenidate is the first-choice medication for the Pervasive Developmental Disorders (PDDs), and comorbid Attention Deficit Hyperactivity Disorder (ADHD). But this approach generally results with poor outcomes, and increased adverse effects. It is aimed to investigate the comparison of cases who diagnosed with PDDs and Mild Mental Retardation (MR) and cases with pure ADHD in terms of the clinical response to MPH. Also we aimed to investigate the relations between CES-1 polymorphism gene and the clinical response to MPH...
2017: Türk Psikiyatri Dergisi, Turkish Journal of Psychiatry
Toshiyuki Nanbu, Naoki Umemura, Emika Ohkoshi, Kumi Nanbu, Hiroshi Sakagami, Jun Shimada
The aim of the present study was to search for an effective regimen among existing chemotherapies for head and neck squamous cell carcinoma (HNSCC). Among the tested drugs, we focused on combined SN-38, which is the active metabolite produced from irinotecan hydrochloride - a type I DNA topoisomerase inhibitor - after it is metabolized by carboxylesterase in the liver and gefitinib, an EGFR tyrosine kinase inhibitor treatment, based on the ability of this combination to inhibit HNSCC cell growth. Contrary to our expectation, in vivo, there was no significant difference in tumor growth suppression between gefitinib-only treatment and gefitinib plus SN-38...
January 2018: Oncology Reports
Hyo-Hyoun Seo, Ae Ran Park, Hyun-Hwa Lee, Sangkyu Park, Yun-Jeong Han, Quyen T N Hoang, Gyung Ja Choi, Jin-Cheol Kim, Yong Soon Kim, Jeong-Il Kim
Colletotrichum species are major fungal pathogens that cause devastating anthracnose diseases in many economically important crops. In this study, we observed the hydrolyzing activity of a fungus-inducible pepper carboxylesterase (PepEST) on cell walls of C. gloeosporioides, causing growth retardation of the fungus by blocking appressorium formation. To determine the cellular basis for the growth inhibition, we observed the localization of PepEST on the fungus and found the attachment of the protein on surfaces of conidia and germination tubes...
November 30, 2017: Molecular Plant-microbe Interactions: MPMI
Qiu-Ling Tang, Kang-Sheng Ma, You-Ming Hou, Xi-Wu Gao
Myzus persicae (Sulzer) is one of the most serious agricultural pests in China, and management strategies mainly rely on insecticidal treatment. To evaluate the resistance of field populations of M. persicae to seven insecticides, we assessed the susceptibility of 11 field populations collected from eight provinces in China using leaf-dip bioassays. Toxicity assays showed that M. persicae field populations have developed several levels of resistance to each tested insecticide. For pyrethroids, the field populations have developed a high level of resistance to β-cypermethrin and cypermethrin, while the resistance to bifenthrin is still low...
November 2017: Pesticide Biochemistry and Physiology
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