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https://www.readbyqxmd.com/read/29753268/bio-activity-of-aminosulfonyl-ureas-in-the-light-of-nucleic-acid-bases-and-dna-base-pair-interaction
#1
Sutapa Mondal Roy
The quantum chemical descriptors based on density functional theory (DFT) are applied to predict the biological activity (log IC50 ) of one class of acyl-CoA: cholesterol O-acyltransferase (ACAT) inhibitors, viz. aminosulfonyl ureas. ACAT are very effective agents for reduction of triglyceride and cholesterol levels in human body. Successful two parameter quantitative structure-activity relationship (QSAR) models are developed with a combination of relevant global and local DFT based descriptors for prediction of biological activity of aminosulfonyl ureas...
April 27, 2018: Computational Biology and Chemistry
https://www.readbyqxmd.com/read/29600657/-effect-of-leech-on-lipid-metabolism-and-liver-in-hyperlipidemia-rats
#2
Jing-Kui Wu, Qiao Yang
To explore the effect of leech on lipid metabolism and liver function in hyperlipidemia rats and the possible mechanism, biochemical analyzer was used to examine the regulation of leech on levels of serum triglycerides(TG), total cholesterol(TC), low-density lipoprotein cholesterol(LDL-C), and high-density lipoprotein cholesterol(HDL-C). The levels of ALT and AST in serum were detected by ELISA. The proteins expression of ACAT-2, Fas and HMGCR in liver tissue was detected by Western blot. The weight of body and liver were weighed, and liver index was calculated...
February 2018: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29593722/formation-of-foamy-macrophages-by-tuberculous-pleural-effusions-is-triggered-by-the-interleukin-10-signal-transducer-and-activator-of-transcription-3-axis-through-acat-upregulation
#3
Melanie Genoula, José Luis Marín Franco, Maeva Dupont, Denise Kviatcovsky, Ayelén Milillo, Pablo Schierloh, Eduardo Jose Moraña, Susana Poggi, Domingo Palmero, Dulce Mata-Espinosa, Erika González-Domínguez, Juan Carlos León Contreras, Paula Barrionuevo, Bárbara Rearte, Marlina Olyissa Córdoba Moreno, Adriana Fontanals, Agostina Crotta Asis, Gabriela Gago, Céline Cougoule, Olivier Neyrolles, Isabelle Maridonneau-Parini, Carmen Sánchez-Torres, Rogelio Hernández-Pando, Christel Vérollet, Geanncarlo Lugo-Villarino, María Del Carmen Sasiain, Luciana Balboa
The ability of Mycobacterium tuberculosis (Mtb) to persist in its human host relies on numerous immune evasion strategies, such as the deregulation of the lipid metabolism leading to the formation of foamy macrophages (FM). Yet, the specific host factors leading to the foamy phenotype of Mtb-infected macrophages remain unknown. Herein, we aimed to address whether host cytokines contribute to FM formation in the context of Mtb infection. Our approach is based on the use of an acellular fraction of tuberculous pleural effusions (TB-PE) as a physiological source of local factors released during Mtb infection...
2018: Frontiers in Immunology
https://www.readbyqxmd.com/read/29588394/the-phospholipase-a-2-pathway-controls-a-synaptic-cholesterol-ester-cycle-and-synapse-damage
#4
Craig Osborne, Ewan West, Clive Bate
The cellular prion protein (PrPC ) acts as a scaffold protein that organises signalling complexes. In synaptosomes, the aggregation of PrPC by amyloid-β (Aβ) oligomers attracts and activates cytoplasmic phospholipase A2 (cPLA2 ) leading to synapse degeneration. The signalling platform is dependent upon cholesterol released from cholesterol esters by cholesterol ester hydrolases (CEH)s. The activation of CEHs depends upon activated cPLA2 and platelet activating factor (PAF) demonstrating a positive feedback system, activated cPLA2 increased cholesterol concentrations, which in turn facilitated cPLA2 activation...
March 27, 2018: Journal of Cell Science
https://www.readbyqxmd.com/read/29549095/in-vitro-exploration-of-acat-contributions-to-lipid-droplet-formation-during-adipogenesis
#5
Yuyan Zhu, Chih-Yu Chen, Junjie Li, Ji-Xin Cheng, Miran Jang, Kee-Hong Kim
As adipose tissue is the major cholesterol storage organ and most of the intracellular cholesterol is distributed to lipid droplets (LDs), cholesterol homeostasis may have a role in the regulation of adipocyte size and function. ACATs catalyze the formation of cholesteryl ester (CE) from free cholesterol to modulate the cholesterol balance. Despite the well-documented role of ACATs in hypercholesterolemia, their role in LD development during adipogenesis remains elusive. Here, we identify ACATs as regulators of de novo lipogenesis and LD formation in murine 3T3-L1 adipocytes...
May 2018: Journal of Lipid Research
https://www.readbyqxmd.com/read/29489864/cholesterol-esterification-inhibition-and-gemcitabine-synergistically-suppress-pancreatic-ductal-adenocarcinoma-proliferation
#6
Junjie Li, Xiaochao Qu, Jie Tian, Jian-Ting Zhang, Ji-Xin Cheng
Recent advances have recognized metabolic reprogramming as an underlying mechanism for cancer drug resistance. However, the role of cholesterol metabolism in drug resistance remain elusive. Herein, we report an increased accumulation of cholesteryl ester in gemcitabine-resistant pancreatic ductal adenocarcinoma (PDAC) cells. A potent inhibitor of acyl-CoA cholesterol acyltransferase-1 (ACAT-1), avasimibe, effectively suppressed proliferation of gemcitabine-resistant PDAC cells. Combination of avasimibe and gemcitabine showed strong synergistic effect in suppressing PDAC cell viability in vitro and tumor growth in vivo...
2018: PloS One
https://www.readbyqxmd.com/read/29469041/natural-extracts-abolished-lipid-accumulation-in-cells-harbouring-non-favourable-pnpla3-genotype
#7
Ángela Rojas, Paloma Gallego, Antonio Gil-Gómez, Rocío Muñoz-Hernández, Lourdes Rojas, Rosario Maldonado, Rocío Gallego, Marta García-Valdecasas, José A Del Campo, Juan D Bautista, Manuel Romero-Gómez
Background & aims. G-allele of PNPLA3 (rs738409) favours triglycerides accumulation and steatosis. In this study, we examined the effect of quercetin and natural extracts from mushroom and artichoke on reducing lipid accumulation in hepatic cells. MATERIAL AND METHODS: Huh7.5 cells were exposed to oleic acid (OA) and treated with quercetin and extracts to observe the lipid accumulation, the intracellular-TG concentration and the LD size. Sterol regulatory element binding proteins-1 (SREBP-1), peroxisome proliferator-activated receptor (PPARα-γ) and cholesterol acyltransferase (ACAT) gene expression levels were analysed...
March 1, 2018: Annals of Hepatology
https://www.readbyqxmd.com/read/29448875/screening-for-cognitive-impairment-in-an-australian-aged-care-assessment-team-as-part-of-comprehensive-geriatric-assessment
#8
Roger Clarnette, Ming Goh, Sneha Bharadwaj, Jillian Ryan, Suzanne Ellis, Anton Svendrovski, D William Molloy, Rónán O'Caoimh
Accurate detection of mild cognitive impairment (MCI) is important to stratify and address risk. Yet, few short cognitive screening instruments are validated for this. . In Australia, all clients referred to an Aged Care Assessment Team (ACAT) receive comprehensive geriatric assessment (CGA) including the Standardized Mini-Mental State Examination (SMMSE). We compared the accuracy of the quick mild cognitive impairment (Qmci) screen to the SMMSE in 283 participants: 195 with dementia, 47 with MCI, and 41 with subjective cognitive decline (SCD) in an Australian community-based ACAT...
February 15, 2018: Neuropsychology, Development, and Cognition. Section B, Aging, Neuropsychology and Cognition
https://www.readbyqxmd.com/read/29404177/a-rare-cause-of-hemoptysis-in-childhood-tracheal-capillary-hemangioma
#9
Mehmet Akif Özgül, Elif Tanrıverdi, Şule Gül, Zehra Yaşar Asuk, Murat Acat, Kenan Abbaslı, Neslihan Akanıl Fener, Erdoğan Çetinkaya
Hemangiomas are benign tumors most frequently seen in childhood and are mostly associated with cutaneous and mucosal surfaces. Tracheal capillary hemangiomas are extremely rare. The most common presenting symptom is hemoptysis, ranging from minor to major and chronic cough. We present the case of a 12-year-old boy with recurrent hemoptysis due to tracheal capillary hemangioma, who was treated with interventional bronchoscopy.
October 2017: Turkish Thoracic Journal
https://www.readbyqxmd.com/read/29390006/altering-lipid-droplet-homeostasis-affects-coxiella-burnetii-intracellular-growth
#10
Minal Mulye, Brianne Zapata, Stacey D Gilk
Coxiella burnetii is an obligate intracellular bacterial pathogen and a causative agent of culture-negative endocarditis. While C. burnetii initially infects alveolar macrophages, it has also been found in lipid droplet (LD)-containing foamy macrophages in the cardiac valves of endocarditis patients. In addition, transcriptional studies of C. burnetii-infected macrophages reported differential regulation of the LD coat protein-encoding gene perilipin 2 (plin-2). To further investigate the relationship between LDs and C...
2018: PloS One
https://www.readbyqxmd.com/read/29381332/structural-and-biochemical-studies-of-substrate-selectivity-in-ascaris-suum-thiolases
#11
Michael R Blaisse, Beverly Fu, Michelle C Y Chang
Thiolases are a class of carbon-carbon bond forming enzymes with important applications in biotechnology and metabolic engineering as they provide a general method for the condensation of two acyl coenzyme A (CoA) substrates. As such, developing a greater understanding of their substrate selectivity would expand our ability to engineer the enzymatic or microbial production of a broad range of small-molecule targets. Here, we report the crystal structures and biochemical characterization of Acat2 and Acat5, two biosynthetic thiolases from Ascaris suum with varying selectivity toward branched compared to linear compounds...
January 30, 2018: Biochemistry
https://www.readbyqxmd.com/read/29282984/cholesterol-oxidase-triton-x-100-parked-microelectrodes-for-the-detection-of-cholesterol-in-plasma-membrane-at-single-cells
#12
Haiyan Xu, Shuai Zhou, Dechen Jiang, Hong-Yuan Chen
The classic electrochemical analysis of plasma membrane cholesterol at single cells utilizes a cholesterol oxidase modified microelectrode that oxidizes local cholesterol efflux from the plasma membrane to generate hydrogen peroxide for the electrochemical quantification. In this letter, a mixture of cholesterol oxidase and Triton X-100 was filled in the microcapillary that could park at the Pt layer coated tip due to slow hydrodynamic flow. During the contact of the tip with the cellular membrane, Triton X-100 at the tip permeabilized the contacted membrane to release cholesterol for the reaction with cholesterol oxidase...
January 16, 2018: Analytical Chemistry
https://www.readbyqxmd.com/read/29234690/the-dataset-describes-phenotypic-changes-induced-by-cholesterol-loading-in-smooth-muscle-cells-isolated-from-the-aortae-of-c57bl-6-mice
#13
Silvia Castiglioni, Matteo Monti, Giuditta Ainis Buscherini, Lorenzo Arnaboldi, Monica Canavesi, Alberto Corsini, Stefano Bellosta
The data presented in this article is related to the research article entitled " ABCA1 and HDL3 are Required to Modulate Smooth Muscle Cells Phenotypic Switch after Cholesterol Loading " (Castiglioni et al., 2017) [1]. This data describes the characterization of the phenotypic changes induced by cholesterol loading in smooth muscle cells (SMCs) isolated from the aortae of C57BL/6 mice. Upon cholesterol loading, there is a significant and concentration-dependent decrease in the expression of Acta2 and a parallel increase in Mac-2, and ATP binding cassette (ABC) transporters Abca1 and Abcg1 ...
February 2018: Data in Brief
https://www.readbyqxmd.com/read/29216726/high-serum-levels-of-igf-i-and-igfbp3-may-increase-comorbidity-risk-for-asthmatic-patients
#14
M Acat, U Toru Erbay, S Sahin, O Arik, C Ayada
OBJECTIVE: Asthma is known as a chronic inflammatory lung disease which has also systemic features. Insulin-like growth factor I (IGF-I) plays a role for asthma pathogenesis. Controversially, IGF-binding protein 3 (IGFBP3) blocks asthma development. That is why IGF-I and IGFBP3 are targeted for future therapeutic treatments of asthma. We aimed to investigate serum level of IGF-I and IGFBP3 in patients with asthma. This study was performed in 27 asthma and 23 healthy individuals. Serum levels of IGF-I and IGFBP3 were measured by human ELISA assay kits...
2017: Bratislavské Lekárske Listy
https://www.readbyqxmd.com/read/29179498/-acat-1-gene-polymorphism-is-associated-with-increased-susceptibility-to-coronary-artery-disease-in-chinese-han-population-a-case-control-study
#15
Yong-Tao Wang, Ying-Hong Wang, Yi-Tong Ma, Zhen-Yan Fu, Yi-Ning Yang, Xiang Ma, Xiao-Mei Li, Dilare Adi, Fen Liu, Bang-Dang Chen
Several studies suggest an important role of Acyl-CoA: cholesterol acyltransferase-1(ACAT-1) in the development of atherosclerosis. The aim of present study was to investigate whether there exists a possible correlation between genetic variations in ACAT-1 genes and coronary artery disease (CAD) risk. Four polymorphisms (rs1044925, rs11545566, rs12121758 and rs10913733) were finally selected and genotyped in 750 CAD patients and 580 health controls, using the improved multiplex ligation detection reaction (iMLDR) method...
October 24, 2017: Oncotarget
https://www.readbyqxmd.com/read/29097185/serum-starvation-of-arpe-19-changes-the-cellular-distribution-of-cholesterol-and-fibulin3-in-patterns-reminiscent-of-age-related-macular-degeneration
#16
Dinusha Rajapakse, Katherine Peterson, Sanghamitra Mishra, Graeme Wistow
Retinal pigment epithelium (RPE) has been implicated as key source of cholesterol-rich deposits at Bruch's membrane (BrM) and in drusen in aging human eye. We have shown that serum-deprivation of confluent RPE cells is associated with upregulation of cholesterol synthesis and accumulation of unesterified cholesterol (UC). Here we investigate the cellular processes involved in this response. We compared the distribution and localization of UC and esterified cholesterol (EC); the age-related macular degeneration (AMD) associated EFEMP1/Fibulin3 (Fib3); and levels of acyl-coenzyme A (CoA): cholesterol acyltransferases (ACAT) ACAT1, ACAT2 and Apolipoprotein B (ApoB) in ARPE-19 cells cultured in serum-supplemented and serum-free media...
December 15, 2017: Experimental Cell Research
https://www.readbyqxmd.com/read/29090229/ctla-4-gene-haplotypes-and-the-risk-of-chronic-hepatitis-c-infection-a-case-control-study
#17
Samaneh Sepahi, Alireza Pasdar, Sina Gerayli, Sina Rostami, Aida Gholoobi, Zahra Meshkat
BACKGROUND: The prevalence of hepatitis C virus (HCV) infection is increasing worldwide. Cytotoxic Tlymphocyte-associated protein 4 ( CTLA-4 ) may play a role in the intensity of the disease. The aim of this study was to evaluate the association between genetic variants of the CTLA-4 and HCV infection. METHODS: Restriction fragment length polymorphism-polymerase chain reaction (RFLP-PCR) was performed as the genotyping assay at four different positions (+49 A>G, -318 C>T, -1722 T>C, and - 1661 A>G)...
October 2017: Reports of Biochemistry & Molecular Biology
https://www.readbyqxmd.com/read/29074218/avasimibe-a-novel-hepatitis-c-virus-inhibitor-that-targets-the-assembly-of-infectious-viral-particles
#18
Longbo Hu, Jinqian Li, Hua Cai, Wenxia Yao, Jing Xiao, Yi-Ping Li, Xiu Qiu, Huimin Xia, Tao Peng
Direct-acting antivirals (DAAs), which target hepatitis C virus (HCV) proteins, have exhibited impressive efficacy in the management of chronic hepatitis C. However, the concerns regarding high costs, drug resistance mutations and subsequent unexpected side effects still call for the development of host-targeting agents (HTAs) that target host factors involved in the viral life cycle and exhibit pan-genotypic antiviral activity. Given the close relationship between lipid metabolism and the HCV life cycle, we investigated the anti-HCV activity of a series of lipid-lowering drugs that have been approved by government administrations or proven safety in clinical trials...
October 23, 2017: Antiviral Research
https://www.readbyqxmd.com/read/29031956/the-solubility-permeability-trade-off-of-progesterone-with-cyclodextrins-under-physiological-conditions-experimental-observations-and-computer-simulations
#19
Le Sun, Bing Zhang, Jin Sun
This study intended to evaluate the effect of cyclodextrins on the apparent solubility and permeability of lipophilic drugs under physiological conditions and establish in silico model to choose the optimal amount of cyclodextrins for cyclodextrin-containing oral formulations. In order to study the effect of cyclodextrins under physiological conditions, bile salts and lecithin were added into the rat intestinal perfusion solution to simulate the fasted intestinal fluid. In addition, the in vivo oral absorption performances of cyclodextrin-containing formulations were simulated by gastrointestinal simulation technology based on the advanced compartmental absorption and transit model...
January 2018: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29028593/genetic-variations-in-the-p11-tpa-bdnf-pathway-are-associated-with-post-stroke-depression
#20
Jinfeng Liang, Yingying Yue, Haitang Jiang, Deqin Geng, Jun Wang, Jianxin Lu, Shenghua Li, Kezhong Zhang, Aiqin Wu, Yonggui Yuan
BACKGROUND: The effects of BDNF on post stroke depression (PSD) may be influenced by genetic variations in intracellular signal transduction pathways, such as the p11/tPA/BDNF pathway. In this study, we aimed to determine the association of polymorphisms in candidate genes of the gene transduction pathway with PSD, as well as the effects of the interactions between genes in our Chinese sample. METHODS: Two-hundred-fifty-four Chinese samples with acute ischaemic stroke included 122 PSD patients and 132 nonPSD patients...
September 29, 2017: Journal of Affective Disorders
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