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https://www.readbyqxmd.com/read/28639358/antilipase-and-antiproliferative-activities-of-novel-fluoroquinolones-and-triazolofluoroquinolones
#1
Shereen Arabiyat, Violet Kasabri, Yusuf Al-Hiari, Yasser K Bustanji, Rabab Albashiti, Ihab M Almasri, Dima A Sabbah
Fluoroquinolones (FQs) have been identified recently as potent inhibitors of pancreatic lipase (PL). The aim of this study is to synthesize novel FQs and triazolofluoroquinolones (TFQs) and to evaluate them in vitro with respect to their antilipolytic efficacy and potency properties. The PL-IC50 values of 12 FQs and TFQs (3 (a-c) - 6 (a-c)) were in the range of 12.5-189.1 μM. These values are further supported by docking studies. The suggested association between obesity and colorectal cancer initiated the evaluation of antiproliferative activity of the new FQs and TFQs against a panel of obesity related colorectal cells (HT29, HCT116, SW620 CACO2 and SW480)...
June 22, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28636207/specificity-of-and-influence-of-hemolysis-lipemia-and-icterus-on-serum-lipase-activity-as-measured-by-the-v-lip-p-slide
#2
Joerg M Steiner, Robynne Gomez, Jan S Suchodolski, Jonathan A Lidbury
BACKGROUND: Measurement of pancreatic lipase in serum is being used for the diagnosis of pancreatitis. OBJECTIVES: The aims of this study were to measure serum lipase activity by the v-LIP-P slide and serum canine pancreatic lipase immunoreactivity (cPLI) concentration by Spec cPL in dogs with exocrine pancreatic insufficiency (EPI) and in serum samples that were hemolyzed, lipemic, or icteric. METHODS: Serum samples from 50 dogs with EPI, 8 samples spiked with canine hemoglobin, Intralipid, or ditaurobilirubin, and 8 samples from dogs with severe hypertriglyceridemia were evaluated using v-LIP-P and Spec cPL assays...
June 21, 2017: Veterinary Clinical Pathology
https://www.readbyqxmd.com/read/28634192/a-new-enzyme-linked-immunosorbent-assay-system-for-human-serum-hepatic-triglyceride-lipase
#3
Kazuya Miyashita, Katsuyuki Nakajima, Isamu Fukamachi, Yuji Muraba, Takafumi Koga, Yohnosuke Shimomura, Tetsuyo Machida, Masami Murakami, Junji Kobayashi
There is no previously established method for measuring human hepatic triglyceride lipase (HTGL) concentration in serum. In this study, we developed new monoclonal antibodies (MoAb mouse 9A1, MoAb rat 141A1) that react with both HTGL in serum and in post-heparin plasma (PHP) and established a novel enzyme-linked immunosorbent assay (ELISA) system for measuring serum HTGL as well as PHP-HTGL concentrations. To confirm the specificity of MoAb, we performed an immunoprecipitation -immunoblotting analysis. Both MoAb mouse 9A1and MoAb rat 141 A1 were able to immunoprecipitate not only recombinant HTGL and PHP-HTGL but also serum HTGL, demonstrating that HTGL exists in serum obtained without heparin injection...
June 20, 2017: Journal of Lipid Research
https://www.readbyqxmd.com/read/28629973/%C3%AE-eleostearic-acid-containing-triglycerides-for-a-continuous-assay-to-determine-lipase-sn-1-and-sn-3-regio-preference
#4
Meddy El Alaoui, Laurent Soulère, Alexandre Noiriel, Yves Queneau, Abdelkarim Abousalham
Lipases are essentially described as sn-1 and sn-3 regio-selective. Actually few methods are available to measure this lipase regio-selectivity, moreover they require chiral chromatography analysis or specific derivations which are discontinuous and time consuming. In this study we describe a new, convenient, sensitive and continuous spectrophotometric method to screen lipases regio-selectivity using synthetic triglycerides (TG) containing α-eleostearic acid (9Z, 11E, 13E-octadecatrienoic acid) either at the sn-1 position [1-α-eleostearoyl-2,3-octadecyl-sn-glycerol (sn-EOO)] or at the sn-3 position [1,2-octadecyl-3-α-eleostearoyl-sn-glycerol (sn-OOE)] and coated onto the wells of microtiter plates...
June 16, 2017: Chemistry and Physics of Lipids
https://www.readbyqxmd.com/read/28619616/activity-independent-screening-of-secreted-proteins-using-split-gfp
#5
Andreas Knapp, Myriam Ripphahn, Kristina Volkenborn, Pia Skoczinski, Karl-Erich Jaeger
The large-scale industrial production of proteins requires efficient secretion, as provided, for instance, by the Sec system of Gram-positive bacteria. Protein engineering approaches to optimize secretion often require the screening of large libraries, e.g. comprising a target protein fused to many different signal peptides. Respective high-throughput screening methods are usually based on photometric or fluorimetric assays enabling fast and simple determination of enzymatic activities. Here, we report on an alternative method for quantification of secreted proteins based on the split GFP assay...
June 12, 2017: Journal of Biotechnology
https://www.readbyqxmd.com/read/28615298/combination-treatment-with-orlistat-containing-nanoparticles-and-taxanes-is-synergistic-and-enhances-microtubule-stability-in-taxane-resistant-prostate-cancer-cells
#6
Joshua J Souchek, Amanda L Davis, Tanner K Hill, Megan B Holmes, Bowen Qi, Pankaj K Singh, Steven J Kridel, Aaron M Mohs
Taxane-based therapy provides a survival benefit in patients with metastatic prostate cancer, yet the median survival is less than 20 months in this setting due in part to taxane-associated resistance. Innovative strategies are required to overcome chemoresistance for improved patient survival. Here, NanoOrl, a new experimental nanoparticle formulation of the FDA-approved drug, orlistat, was investigated for its cytotoxicity in taxane-resistant prostate cancer utilizing two established taxane-resistant (TxR) cell lines...
June 14, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28613438/uhplc-esi-hr-ms-ms-profiling-of-phenolics-from-tunisian-lycium-arabicum-boiss-antioxidant-and-anti-lipase-activities-evaluation
#7
Marwa Affes, Jawhar Fakhfakh, Ines Douad, Vincent Brieudes, Maria Halabalaki, Abdelfattah El Feki, Noureddine Allouche
This study was performed in the aim to evaluate 9 different extracts from Tunisian L. arabicum for their total phenolic (TPC) and total flavonoid (TFC) contents, phytochemical analyses as well as their antioxidant and anti-lipase activities. The in vitro antioxidant property was investigated using three complementary methods (DPPH, Ferric reducing antioxidant capacity (FRAP) and β-carotene-linoleic acid bleaching assays) while anti-lipase activity was evaluated using 4-methylumbelliferyl oleate method. From all of the tested extracts the most potent found to be the polar methanol extracts especially those of stems and leaves...
June 14, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/28607028/chemoenzymatic-synthesis-nanotization-and-anti-aspergillus-activity-of-optically-enriched-fluconazole-analogues
#8
Shashwat Malhotra, Seema Singh, Neha Rana, Shilpi Tomar, Priyanka Bhatnagar, Mohit Gupta, Suraj K Singh, Brajendra K Singh, Anil K Chhillar, Ashok K Prasad, Christophe Len, Pradeep Kumar, Kailash C Gupta, Anjani J Varma, Ramesh C Kuhad, Gainda L Sharma, Virinder S Parmar, Nigel G J Richards
Despite recent advances in diagnostic and therapeutic advances in antifungal research, aspergillosis still remains a leading cause of morbidity and mortality. One strategy to address this problem is to enhance the activity spectrum of known antifungals, and we now report the first successful application of Candida antarctica lipase (CAL) for the preparation of optically enriched fluconazole analogs. Anti-Aspergillus activity was observed for an optically enriched derivative, (-)-S-2-(2' ,4' -difluorophenyl)-1-hexyl-amino-3-(1‴,2‴,4‴) triazol-1‴-yl-propan-2-ol, which exhibits MIC values of 15...
June 12, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28570839/mir-26b-promotes-3t3-l1-adipocyte-differentiation-through-targeting-pten
#9
Guilin Li, Chunyou Ning, Yao Ma, Long Jin, Qianzi Tang, Xuewei Li, Mingzhou Li, Haifeng Liu
microRNAs (miRNAs) play important roles in adipogenesis that is closely linked to obesity and energy homeostasis. Thus far, only a few miRNAs have been identified to regulate adipocyte development, arousing interest in the detailed function of miRNAs during adipogenesis. In this study, we found that the miR-26b expression showed an increasing trend during 3T3-L1 cells differentiation. To investigate the role of miR-26b in adipogenesis, the synthetic miR-26b agomirs and antagomirs were used to perform overexpression and knockdown experiment, respectively...
June 1, 2017: DNA and Cell Biology
https://www.readbyqxmd.com/read/28539721/phytochemical-and-biological-evaluations-of-arum-hygrophilum-boiss-araceae
#10
Fatma U Afifi, Violet Kasabri, Simona Litescu, Ismail F Abaza, Khalid Tawaha
BACKGROUND: Arum hygrophilum is a traditional medicinal plant indigenous to Jordan. The present study explores its phytochemistry, antioxidative, antidiabesity, and antiproliferative potentialities. MATERIALS AND METHODS: Column chromatography and HPLC-MS analysis were used for its phytochemical evaluation. Using leaf crude water and ethanol extracts, the antioxidative capacities, their modulation of pancreatic β-cell proliferation, and insulin secretion as well as glucose diffusion and enzymatic bioassays were evaluated...
April 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28534980/a-proteomic-analysis-identifies-candidate-early-biomarkers-to-predict-ovarian-hyperstimulation-syndrome-in-polycystic-ovarian-syndrome-patients
#11
Lan Wu, Yazhou Sun, Jun Wan, Ting Luan, Qing Cheng, Yong Tan
Ovarian hyperstimulation syndrome (OHSS) is a potentially life‑threatening, iatrogenic complication that occurs during assisted reproduction. Polycystic ovarian syndrome (PCOS) significantly increases the risk of OHSS during controlled ovarian stimulation. Therefore, a more effective early prediction technique is required in PCOS patients. Quantitative proteomic analysis of serum proteins indicates the potential diagnostic value for disease. In the present study, the authors revealed the differentially expressed proteins in OHSS patients with PCOS as new diagnostic biomarkers...
July 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28534439/hypolipidemic-and-hepatoprotective-activities-of-rosemary-and-thyme-in-gentamicin-treated-rats
#12
A M Hegazy, A S Abdel-Azeem, H M Zeidan, K S Ibrahim, Em El Sayed
Rosemary ( Rosmarinus officinalis; RM) and thyme ( Thymus vulgaris; TV) are used as remedies. We designed this work to investigate the preventive effect of aqueous extracts of RM or TV on the gentamicin (GM)-induced hepatotoxicity and abnormalities of lipid profile in rats. Both plant extracts exhibited an in vitro antioxidant activity as determined by the 1,1-diphenyl-2-picrylhydrazyl assay. Radical scavenging activity for TV extract was 48.7% and for RM extract was 25.6%. Polyphenolic determination by high-performance liquid chromatography for both extracts revealed that catechin, coumarin, cinnamic acid and rutin were detected in both extracts...
January 1, 2017: Human & Experimental Toxicology
https://www.readbyqxmd.com/read/28532785/best-practice-in-the-measurement-and-interpretation-of-lysosomal-acid-lipase-in-dried-blood-spots-using-the-inhibitor-lalistat-2
#13
Zoltan Lukacs, Marianne Barr, John Hamilton
Lysosomal acid lipase deficiency (LAL-D) is an inherited, autosomal recessive lysosomal storage disorder characterized by progressive damage in multiple organ systems. Diagnosis is especially important in infants, in whom the course of disease is rapidly lethal without treatment. The recent regulatory approval of recombinant human lysosomal acid lipase (LAL), sebelipase alfa, merits rapid diagnosis in clinical routine, particularly in infants. A method for measuring LAL activity in dried blood spot (DBS) samples using the highly specific LAL inhibitor Lalistat 2 is available...
May 19, 2017: Clinica Chimica Acta; International Journal of Clinical Chemistry
https://www.readbyqxmd.com/read/28512098/a-rare-case-of-thrombotic-microangiopathy-triggered-by-acute-pancreatitis
#14
Kevin Singh, Ahmed Jamal Nadeem, Behzad Doratotaj
Thrombotic microangiopathy (TMA) occurring after acute pancreatitis is rarely described. Without prompt intervention, TMA can be, and often is, lethal, so prompt recognition is important. Here, we present a case of a 61-year-old woman with a history of alcohol misuse who presented with epigastric pain, nausea and vomiting after binge drinking. Elevated serum lipase and imaging were suggestive of acute-on-chronic pancreatitis. Although the patient's symptoms of acute pancreatitis subsided, her anaemia, thrombocytopenia and acute kidney injury worsened...
May 15, 2017: BMJ Case Reports
https://www.readbyqxmd.com/read/28488138/enantioselective-resolution-of-racemic-flurbiprofen-methyl-ester-by-lipase-encapsulated-mercapto-calix-4-arenes-capped-fe3o4-nanoparticles
#15
Hasan Yildiz, Elif Ozyilmaz, Asif Ali Bhatti, Mustafa Yilmaz
This work presents the synthesis of new mercapto calix[4]arenes derivatives (4 and 5). These derivatives were capped on Fe3O4 magnetic nanoparticles and subsequently encapsulated with Candida rugosa through sol-gel method to furnish enc-4 and enc-5, respectively, to enhance catalytic activity and enantioselectivity of lipase for hydrolysis reaction of racemic flurbiprofen methyl ester. Catalytic activity and enantioselectivity of enc-4 and enc-5 were assayed at different pH and temperature conditions and it was found that the resultant encapsulated enzyme exhibited higher thermal and operational stabilities compared to the free lipase in which enc-5 showed the excellent rate of enantioselectivity (E = 176) for S-flurbiprofen better than free lipase (E = 137) at pH 7 and 35 °C for 48 h...
May 9, 2017: Bioprocess and Biosystems Engineering
https://www.readbyqxmd.com/read/28480147/effect-of-the-molecular-weight-of-water-soluble-chitosan-on-its-fat-cholesterol-binding-capacities-and-inhibitory-activities-to-pancreatic-lipase
#16
Qiu Jin, Huahua Yu, Xueqin Wang, Kecheng Li, Pengcheng Li
BACKGROUND: Obesity has become a worldwide burden to public health in recent decades. Given that obesity is caused by an imbalance between caloric intake and expenditure, and that dietary fat is the most important energy source of all macronutrients (by providing the most calories), a valuable strategy for obesity treatment and prevention is to block fat absorption via the gastrointestinal pathway. In this study, the fat- and cholesterol-binding capacities and the inhibition of pancreatic lipase by water-soluble chitosan (WSC) with different weight-average molecular weight (Mw) were tested and compared in vitro, in order to determine the anti-obesity effects of WSC and the influence of its Mw...
2017: PeerJ
https://www.readbyqxmd.com/read/28479718/potential-lipid-lowering-effects-of-eleusine-indica-l-gaertn-extract-on-high-fat-diet-induced-hyperlipidemic-rats
#17
Siew Ling Ong, Koteswara Rao Nalamolu, How Yee Lai
BACKGROUND: To date, anti-obesity agents based on natural products are tested for their potential using lipase inhibition assay through the interference of hydrolysis of fat by lipase resulting in reduced fat absorption without altering the central mechanisms. Previous screening study had indicated strong anti-obesity potential in Eleusine indica (E. indica), but to date, no pharmacologic studies have been reported so far. OBJECTIVE: This study was performed to investigate the lipid-lowering effects of E...
January 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28465058/establishment-and-application-of-a-modified-membrane-blot-assay-for-rhizomucor-miehei-lipases-aimed-at-improving-their-methanol-tolerance-and-thermostability
#18
Dong He, Wen Luo, Zhiyuan Wang, Pengmei Lv, Zhenhong Yuan, Shaowei Huang, Jingliang Xv
Directed evolution has been proved an effective way to improve the stability of proteins, but high throughput screening assays for directed evolution with simultaneous improvement of two or more properties are still rare. In this study, we aimed to establish a membrane-blot assay for use in the high-throughput screening of Rhizomucor miehei lipases (RMLs). With the assistance of the membrane-blot screening assay, a mutant E47K named G10 that showed improved thermal stability was detected in the first round of error-prone PCR...
July 2017: Enzyme and Microbial Technology
https://www.readbyqxmd.com/read/28459005/discovery-and-characterizaton-of-a-novel-lipase-with-transesterification-activity-from-hot-spring-metagenomic-library
#19
Wei Yan, Furong Li, Li Wang, Yaxin Zhu, Zhiyang Dong, Linhan Bai
A new gene encoding a lipase (designated as Lip-1) was identified from a metagenomic bacterial artificial chromosome(BAC) library prepared from a concentrated water sample collected from a hot spring field in Niujie, Eryuan of Yunnan province in China. The open reading frame of this gene encoded 622 amino acid residues. It was cloned, fused with the oleosin gene and over expressed in Escherichia coli to prepare immobilized lipase artificial oil body AOB-sole-lip-1. The monomeric Sole-lip-1 fusion protein presented a molecular mass of 102...
March 2017: Biotechnology Reports
https://www.readbyqxmd.com/read/28448467/chemical-composition-and-biological-activities-of-mono-and-heterofloral-bee-pollen-of-different-geographical-origins
#20
Jucilene Silva Araújo, Emerson Dechechi Chambó, Maria Angélica Pereira de Carvalho Costa, Samira Maria Peixoto Cavalcante da Silva, Carlos Alfredo Lopes de Carvalho, Leticia M Estevinho
Recent research shows variations in pollen chemical constituents and, consequently, in their therapeutic properties. Mono and multifloral bee pollen extracts were investigated for antioxidant and enzyme inhibitory activity properties, phenolic compounds and fatty acid composition. Generally, Eucalyptus spp. and multifloral extracts exhibited potent inhibitory activity against α-amylase, acetylcholinesterase, tyrosinase, lipoxygenase, lipase and hyaluronidase. On the other hand, Miconia spp. demonstrated higher antihemolytic activity...
April 27, 2017: International Journal of Molecular Sciences
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