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https://www.readbyqxmd.com/read/28809813/molecular-mechanisms-underlying-inhibitory-binding-of-alkylimidazolium-ionic-liquids-to-laccase
#1
Jianliang Sun, Hao Liu, Wenping Yang, Shicheng Chen, Shiyu Fu
Water-miscible alkylimidazolium ionic liquids (ILs) are "green" co-solvents for laccase catalysis, but generally inhibit enzyme activity. Here, we present novel insights into inhibition mechanisms by a combination of enzyme kinetics analysis and molecular simulation. Alkylimidazolium cations competitively bound to the TI Cu active pocket in the laccase through hydrophobic interactions. Cations with shorter alkyl chains (C₂~C₆) entered the channel inside the pocket, exhibiting a high compatibility with laccase (competitive inhibition constant Kic = 3...
August 15, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28809474/a-nano-in-nano-approach-for-enzyme-immobilization-based-on-block-copolymers
#2
Finizia Auriemma, Claudio De Rosa, Anna Malafronte, Rocco Di Girolamo, Chiara Santillo, Yuri Gerelli, Giovanna Fragneto, Robert David Barker, Vincenzo Pavone, Ornella Maglio, Angela Lombardi
We have set-up a facile approach for fabrication of supports with tailored nanoporosity for immobilization of enzymes. To this aim block copolymers self-assembly has been used to prepare nanostructured thin films with well-defined architecture containing pores of tailorable size delimited by walls with tailorable degree of hydrophilicity. In particular, we have employed a mixture of polystyrene-block-poly(L-lactide) (PS-PLLA) and polystyrene-block-poly(ethylene oxide) (PS-PEO) diblock copolymers to generate thin films with a lamellar morphology consisting of PS lamellar do-mains alternating with mixed PEO/PLLA blocks lamellar domains...
August 15, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28808388/caesalpinia-crista-linn-induces-protection-against-dna-and-membrane-damage
#3
R Sunil Kumar, Ramesh Balenahalli Narasingappa, Chandrashekhar G Joshi, Talakatta K Girish, Ananda Danagoudar
BACKGROUND: Caesalpinia crista is a medicinal herb used to cure various ailments in subtropical and tropical regions of Southeast Asia. OBJECTIVE: The objective of this evaluation of C. crista against free radical induced DNA and erythrocyte damage. MATERIALS AND METHODS: The profiles of polyphenol and flavonoid were quantified through reversed-phase high-performance liquid chromatography. Free radical induced DNA and membrane damage were performed using H2O2 as oxidative agent...
July 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28808381/characterization-antibacterial-and-antioxidant-properties-of-silver-nanoparticles-synthesized-from-aqueous-extracts-of-allium-sativum-zingiber-officinale-and-capsicum-frutescens
#4
Gloria Aderonke Otunola, Anthony Jide Afolayan, Emmanuel Olusegun Ajayi, Samuel Wale Odeyemi
BACKGROUND: Herbal drug delivery is limited by poor solubility and bioavailability which can be overcome with suitable nanomaterials that will enhance their pharmacokinetics and performance. OBJECTIVE: This study aimed to analyze the synthesis, characterization, and biological activities of silver nanoparticles (AgNPs) from three spices. MATERIALS AND METHODS: AgNPs were prepared using 0.1 M silver nitrate and aqueous extracts of Allium sativum L...
July 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28808226/atr-inhibition-facilitates-targeting-of-leukemia-dependence-on-convergent-nucleotide-biosynthetic-pathways
#5
Thuc M Le, Soumya Poddar, Joseph R Capri, Evan R Abt, Woosuk Kim, Liu Wei, Nhu T Uong, Chloe M Cheng, Daniel Braas, Mina Nikanjam, Peter Rix, Daria Merkurjev, Jesse Zaretsky, Harley I Kornblum, Antoni Ribas, Harvey R Herschman, Julian Whitelegge, Kym F Faull, Timothy R Donahue, Johannes Czernin, Caius G Radu
Leukemia cells rely on two nucleotide biosynthetic pathways, de novo and salvage, to produce dNTPs for DNA replication. Here, using metabolomic, proteomic, and phosphoproteomic approaches, we show that inhibition of the replication stress sensing kinase ataxia telangiectasia and Rad3-related protein (ATR) reduces the output of both de novo and salvage pathways by regulating the activity of their respective rate-limiting enzymes, ribonucleotide reductase (RNR) and deoxycytidine kinase (dCK), via distinct molecular mechanisms...
August 14, 2017: Nature Communications
https://www.readbyqxmd.com/read/28807904/no-clinically-relevant-drug-drug-interactions-between-methadone-or-buprenorphine-naloxone-and-anti-viral-combination-glecaprevir-and-pibrentasvir
#6
Matthew Kosloski, Weihan Zhao, Armen Asatryan, Jens Kort, Pierre Geoffroy, Wei Liu
The combination of glecaprevir (formerly ABT-493), a nonstructural (NS) protein 3/4A protease inhibitor, and pibrentasvir (formerly ABT-530), a NS5A protein inhibitor, is being developed as treatment for HCV genotype 1-6 infection. The pharmacokinetics, pharmacodynamics, safety, and tolerability of methadone or buprenorphine/naloxone when coadministered with the glecaprevir and pibrentasvir combination in HCV-negative subjects on stable opioid maintenance therapy were investigated in a Phase 1, single-center, two-arm, multiple-dose, open-label sequential study...
August 14, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28806222/transient-receptor-potential-vanilloid-1-antagonists-prevent-anesthesia-induced-hypothermia-and-decrease-postincisional-opioid-dose-requirements-in-rodents
#7
Andras Garami, Mohab Ibrahim, Kerry Gilbraith, Rajesh Khanna, Eszter Pakai, Alexandra Miko, Erika Pinter, Andrej A Romanovsky, Frank Porreca, Amol M Patwardhan
BACKGROUND: Intraoperative hypothermia and postoperative pain control are two important clinical challenges in anesthesiology. Transient receptor potential vanilloid 1 has been implicated both in thermoregulation and pain. Transient receptor potential vanilloid 1 antagonists were not advanced as analgesics in humans in part due to a side effect of hyperthermia. This study tested the hypothesis that a single, preincision injection of a transient receptor potential vanilloid 1 antagonist could prevent anesthesia-induced hypothermia and decrease the opioid requirement for postsurgical hypersensitivity...
August 14, 2017: Anesthesiology
https://www.readbyqxmd.com/read/28806057/rational-design-and-multi-biological-profiling-of-novel-donepezil-trolox-hybrids-against-alzheimer-s-disease-with-cholinergic-antioxidant-neuroprotective-and-cognition-enhancing-properties
#8
Pei Cai, Si-Qiang Fang, Xue-Lian Yang, Jia-Jia Wu, Qiao-Hong Liu, Hao Hong, Xiao-Bing Wang, Lingyi Kong
A novel series of donepezil-trolox hybrids were designed, synthesized and evaluated as multifunctional ligands against Alzheimer's disease (AD). Biological assays showed that these derivatives possessed moderate to good inhibitory activities against acetylcholinesterase (AChE) and monoamine oxidase B (MAO-B) as well as remarkable antioxidant effects. The optimal compound 6d exhibited balanced functions with good inhibition against hAChE (IC50 = 0.54 μM) and hMAO-B (IC50 = 4.3 μM), significant antioxidant activity (41...
August 14, 2017: ACS Chemical Neuroscience
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
#9
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/28804435/color-anthocyanin-and-antioxidant-characteristics-of-young-wines-produced-from-spine-grapes-vitis-davidii-foex-in-china
#10
Fuliang Han, Yanlun Ju, Xianrui Ruan, Xianfang Zhao, Xiaofeng Yue, Xifu Zhuang, Minyang Qin, Yulin Fang
Background: Spine grape has gained attention in the field of wine science due to its good growth characteristics. Spine grape wine has been made by local residents for a long time. However, the scientific evaluation of spine wine has not been systemically documented compared to Vitis vinifera grape wines Methods: We compared 11 spine wines from south China (W1-W11) with 7 high-quality international wines (W12-W18). The total phenolic content, the total anothcyanin content and the antioxidant activity of these wines were analyzed and compared...
2017: Food & Nutrition Research
https://www.readbyqxmd.com/read/28803117/phenolics-from-rubus-fairholmianus-induces-cytotoxicity-and-apoptosis-in-human-breast-adenocarcinoma-cells
#11
Blassan P George, Heidi Abrahamse, Nanjundaswamy M Hemmaragala
Herbal medicine is an important part of health care system in most of the countries. Rubus fairholmianus is an unexplored berry in folkloric medicine. In this study, we aimed to understand the importance of R. fairholmianus in pharmaceutical industry for the development of cost-effective cancer therapeutic drugs using in vivo and in vitro analysis. Chemical characterisation, antioxidant, antiproliferative and apoptosis inducing properties of R. fairholmianus root methanolic column subfraction (RFM) were investigated...
August 9, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28799432/targeted-therapies-in-acute-myeloid-leukemia-a-focus-on-flt-3-inhibitors-and-abt199
#12
Kiran Naqvi, Marina Konopleva, Farhad Ravandi
Acute myeloid leukemia (AML) remains a therapeutic challenge. Despite ongoing research, the standard therapy for AML has not changed significantly in the past four decades. With the identification of cytogenetic and molecular abnormalities, several promising therapeutic agents are currently being investigated. FLT3 mutation is a well-recognized target seen in 30% of the cytogenetically normal AML. More recently, the BCL2 family of anti-apoptotic proteins have also generated great interest as a therapeutic target...
August 11, 2017: Expert Review of Hematology
https://www.readbyqxmd.com/read/28798337/the-laccase-like-reactivity-of-manganese-oxide-nanomaterials-for-pollutant-conversion-rate-analysis-and-cyclic-voltammetry
#13
Xinghao Wang, Jiaoqin Liu, Ruijuan Qu, Zunyao Wang, Qingguo Huang
Nanostructured manganese oxides, e.g. MnO2, have shown laccase-like catalytic activities, and are thus promising for pollutant oxidation in wastewater treatment. We have systematically compared the laccase-like reactivity of manganese oxide nanomaterials of different crystallinity, including α-, β-, γ-, δ-, and ɛ-MnO2, and Mn3O4, with 2,2'-azinobis-(3-ethylbenzthiazoline-6-sulfonate) (ABTS) and 17β-estradiol (E2) as the probing substrates. The reaction rate behaviors were examined with regard to substrate oxidation and oxygen reduction to evaluate the laccase-like catalysis of the materials, among which γ-MnO2 exhibits the best performance...
August 10, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28798075/cytokines-of-the-il-1-family-recognized-targets-in-chronic-inflammation-underrated-in-organ-transplantations
#14
REVIEW
Ilja Striz
Interleukin 1 (IL-1) family is a group of cytokines with multiple local and systemic effects, which regulates both innate and adaptive immune responses. Generally, most IL-1 family cytokines express prevailing pro-inflammatory activities (IL-1α, IL-1β, IL-18, IL-33, IL-36 α, β, γ), whereas others are anti-inflammatory (IL-1Ra (IL-1 receptor antagonist), IL-36Ra, IL-38, IL-37). In addition to their immunomodulatory roles, some of them are also involved in the physiological modulation of homeostatic processes and directly affect mRNA transcription...
September 1, 2017: Clinical Science (1979-)
https://www.readbyqxmd.com/read/28797651/biological-effects-and-chemical-characterization-of-iris-schachtii-markgr-extracts-a-new-source-of-bioactive-constituents
#15
Andrei Mocan, Gokhan Zengin, Adriano Mollica, Ahmet Uysal, Erdogan Gunes, Gianina Crișan, Abdurrahman Aktumsek
This study gathers information about the effects of different extracts (methanol and water) from rhizomes and aerial parts of Iris schachtii on selected enzymes (cholinesterases, alpha-amylase and alpha-glucosidase, tyrosinase and lipase) as well as on their antioxidant capacities and antimutagenic properties in relation with their phenolic composition. The chemical composition was assessed by determining total phenolic and flavonoid content as well as individual phenolic compounds by HPLC-DAD. Moreover, antioxidant abilities of the investigated extracts were tested by using different assays including free radical scavenging (DPPH and ABTS), reducing power (CUPRAC and FRAP), phosphomolybdenum and metal chelating, overall rhizomes being indicated as a superior source of antioxidant compounds...
August 7, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28791718/dried-blood-spots-from-finger-prick-facilitate-therapeutic-drug-monitoring-of-adalimumab-and-anti-adalimumab-in-patients-with-inflammatory-diseases
#16
E L Kneepkens, M F Pouw, G J Wolbink, T Schaap, M T Nurmohamed, A de Vries, T Rispens, K Bloem
BACKGROUND: Development of a self-sampling method for therapeutic drug monitoring (TDM) of biologicals will enhance TDM implementation in routine care and pharmacokinetic knowledge. AIM: To compare adalimumab and anti-adalimumab antibody (ADA) concentration measurements in dried blood spots (DBS) obtained from finger prick with measurements in serum obtained via venepuncture, from patients with rheumatic inflammatory diseases. METHODS: In this cross-sectional study, 161 consecutive patients were included...
August 9, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28783849/multiple-measures-are-needed-to-quantify-training-loads-in-professional-rugby-league
#17
Daniel Weaving, Ben Jones, Phil Marshall, Kevin Till, Grant Abt
This study aims to investigate the effect of training mode (conditioning and skills) on multivariate training load relationships in professional rugby league via principal component analysis. Four measures of training load (internal: heart rate exertion index, session rating of perceived exertion; external: PlayerLoad™, individualised high-speed distance) were collected from 23 professional male rugby league players over the course of one 12 wk preseason period. Training was categorised by mode (skills or conditioning) and then subjected to a principal component analysis...
August 7, 2017: International Journal of Sports Medicine
https://www.readbyqxmd.com/read/28783112/optimization-of-the-ultrasound-assisted-extraction-of-phenolic-compounds-from-brosimum-alicastrum-leaves-and-the-evaluation-of-their-radical-scavenging-activity
#18
Mariel Gullian Klanian, Montserrat Terrats Preciat
In order to maximize the yield of the total phenolic content (TPC) and total monomeric anthocyanin (TMA) from Brosimum alicastrum leaf and to study the radical-scavenging activity, a three-level three-factor Box-Behnken design (BBD) was used to determine the optimal points for ultrasound-assisted extraction (UAE). In this study, we analyzed the extraction time (10, 20, and 30 min), temperature (28, 30, and 32 °C), and probe sonication power (40%, 28 W/cm²; 60%, 51 W/cm²; and 80%, 74 W/cm²). Analysis of variance (ANOVA) indicated that the sonication power plays a significant role in the extraction of phenolic compounds...
August 7, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28782382/attentional-biases-for-threat-after-fear-related-autobiographical-recall
#19
Laura Sagliano, Luigi Trojano, Valentina Di Mauro, Paola Carnevale, Marina Di Domenico, Caterina Cozzolino, Francesca D'Olimpio
BACKGROUND: Previous studies suggested that affective state could enhance stimulus salience and modulate attention allocation for mood-congruent information, but contrasting data have been reported on the effects of mood induction on attentional biases for threat (ABTs) in non-clinical individuals. OBJECTIVE: We aimed to assess whether laboratory-induced negative mood can increase individuals' tendency to allocate attention on threatening stimuli, thus determining a difficulty in attentional disengagement from threat...
August 7, 2017: Anxiety, Stress, and Coping
https://www.readbyqxmd.com/read/28782244/using-the-affective-bias-test-to-predict-drug-induced-negative-affect-implications-for-drug-safety
#20
S A Stuart, C M Wood, E S J Robinson
BACKGROUND AND PURPOSE: Predicting the risk of drug-induced adverse psychiatric effects is important but currently not possible in non-human species. This study has investigated whether the affective bias test (ABT) could provide a preclinical method with translational and predictive validity. EXPERIMENTAL APPROACH: The ABT is a bowl-digging task which quantifies biases associated with learning and memory. Rats encounter independent learning experiences, on separate days, under either acute manipulations (e...
August 7, 2017: British Journal of Pharmacology
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