Read by QxMD icon Read


Meghan MacKenzie, Richard Hall
PURPOSE: Knowledge of how alterations in pharmacogenomics and pharmacogenetics may affect drug therapy in the intensive care unit (ICU) has received little study. We review the clinically relevant application of pharmacogenetics and pharmacogenomics to drugs and conditions encountered in the ICU. SOURCE: We selected relevant literature to illustrate the important concepts contained within. PRINCIPAL FINDINGS: Two main approaches have been used to identify genetic abnormalities - the candidate gene approach and the genome-wide approach...
October 17, 2016: Canadian Journal of Anaesthesia, Journal Canadien D'anesthésie
Fábio de Melo Tarouco, Filipe Guilherme Andrade de Godoi, Robson Rabelo Velasques, Amanda da Silveira Guerreiro, Marcio Alberto Geihs, Carlos Eduardo da Rosa
Glyphosate based herbicides, including Roundup, are widely employed in agriculture and urban spaces. The objective of this study was to evaluate the toxicological effects of Roundup on the estuarine polychaeta Laeonereis acuta. Biomarkers of oxidative stress as well as acetylcholinesterase and propionilcholinesterase activities were analyzed. Firstly, the LC50 96h for L. acuta was established (8.19mg/L). After, the animals were exposed to two Roundup concentrations: 3.25mg/L (non-observed effect concentration - NOEC) and 5...
October 14, 2016: Ecotoxicology and Environmental Safety
Juliana Maria de Mello Andrade, Natasha Maurmann, Patricia Pranke, Izabel Cristina Casanova Turatti, Norberto Peporine Lopes, Amélia T Henriques
OBJECTIVES: The hexane (HEX) and dichloromethane (DCM) fractions from Blechnum binervatum, Blechnum brasiliense and Blechnum occidentale were studied about phytochemicals and biological properties using multitarget approach. METHODS: The chemical composition was performed by gas chromatography coupled with mass spectrometry detector (GC-MS) analysis. Antioxidant capacity was evaluated against free radicals and on lipid peroxidation. Monoamine oxidases (MAO) and cholinesterases enzymatic modulation, as well as effects on rat and human cells, were assessed...
October 17, 2016: Journal of Pharmacy and Pharmacology
Carlos Silva, Bruno Nunes, António Ja Nogueira, Fernando Gonçalves, Joana L Pereira
Using the bivalve macrofouler Corbicula fluminea, the suitability of in vitro testing as a stepping stone towards the improvement of control methods based on chemical mixtures was addressed in this study. In vitro cholinesterase (ChE) activity inhibition following single exposure of C. fluminea tissue to four model chemicals (the organophosphates dimethoate and dichlorvos, copper and sodium dodecyl phosphate [SDS]) was first assessed. Consequently, mixtures of dimethoate with copper and dichlorvos with SDS were tested and modelled; mixtures with ChE revealed synergistic interactions for both chemical pairs...
November 2016: Biofouling
Jacques Joubert, Germaine B Foka, Benjamin P Repsold, Douglas W Oliver, Erika Kapp, Sarel F Malan
A series of 7-substituted coumarin derivatives were designed and synthesised to display ChE and MAO-B inhibitory activity. The compounds consisted out of a coumarin structure (MAO-B inhibitor) and benzyl-, piperidine-, N-benzylpiperidine- or p-bromo-N-benzylpiperizine moiety, resembling the N-benzylpiperidine function of donepezil (ChE inhibitor), connected via an alkyl ether linkage at the 7 position. The biological assay results indicated that all the compounds (1-25) displayed selective inhibition to hMAO-B over hMAO-A, with the benzyloxy series (1-8, 10-13) showing nano-molar hMAO-B inhibition (IC50: 0...
September 15, 2016: European Journal of Medicinal Chemistry
Jie Wu, Yiguang Tian, Shanping Wang, Marco Pistolozzi, Ya Jin, Ting Zhou, Gaurab Roy, Ling Xu, Wen Tan
An increase activity of butyrylcholinesterase is believed to contribute to Alzheimer's disease. Bambuterol is a known potent inhibitor of butyrylcholinesterase, but it has undesired cardiac effects and less lipophilicity. Thirteen bambuterol analogues were synthesized using 1-(3, 5-dihydroxyphenyl) ethanone as a starting material. In-vitro cholinesterase assay established that the majority of the compounds are specific butyrylcholinesterase inhibitors. Out of the 13 compounds, two bambuterol derivatives, BD-6 and BD-11 exhibited similar efficacies in inhibiting butyrylcholinesterase with fewer effects on heart and enhanced possibilities of permeating through the blood-brain barrier as compared to bambuterol...
August 26, 2016: European Journal of Medicinal Chemistry
Koji Hori, Kimiko Konishi, Misa Hosoi, Hiroi Tomioka, Masayuki Tani, Yuka Kitajima, Mitsugu Hachisu
Given the relationship between anticholinergic activity (AA) and Alzheimer's disease (AD), we rereview our hypothesis of the endogenous appearance of AA in AD. Briefly, because acetylcholine (ACh) regulates not only cognitive function but also the inflammatory system, when ACh downregulation reaches a critical level, inflammation increases, triggering the appearance of cytokines with AA. Moreover, based on a case report of a patient with mild AD and slightly deteriorated ACh, we also speculate that AA can appear endogenously in Lewy body disease due to the dual action of the downregulation of ACh and hyperactivity of the hypothalamic-pituitary-adrenal axis...
2016: Parkinson's Disease
Minzhen Deng, Liping Huang, Baile Ning, Nanbu Wang, Qinxin Zhang, Caixia Zhu, Yongqi Fang
Alzheimer's disease (AD) is the most common neurodegenerative disorder in the elderly, and studies have suggested that β-asarone has pharmacological effects on beta-amyloid (Aβ) injected in the rat hippocampus. However, the effect of β-asarone on autophagy in the APP/PS1 transgenic mouse is unreported. APP/PS1 transgenic mice were randomly divided into six groups (n=10/group): an untreated group, an Aricept-treated group, a 3-MA-treated group, a rapamycin-treated group, an LY294002-treated group, a β-asarone-treated group...
October 10, 2016: Brain Research
Ziwei Chen, Maria Digiacomo, Yalin Tu, Qiong Gu, Shengnan Wang, Xiaohong Yang, Jiaqi Chu, Qiuhe Chen, Yifan Han, Jingkao Chen, Giulia Nesi, Simona Sestito, Marco Macchia, Simona Rapposelli, Rongbiao Pi
A series of rivastigmine-caffeic acid and rivastigmine-ferulic acid hybrids were designed, synthesized, and evaluated as multifunctional agents for Alzheimer's disease (AD) in vitro. The new compounds exerted antioxidant neuroprotective properties and good cholinesterases (ChE) inhibitory activities. Some of them also inhibited amyloid protein (Aβ) aggregation. In particular, compound 5 emerged as promising drug candidates endowed with neuroprotective potential, ChE inhibitory, Aβ self-aggregation inhibitory and copper chelation properties...
September 17, 2016: European Journal of Medicinal Chemistry
Mohamed Benchekroun, Alejandro Romero, Javier Egea, Rafael León, Patrycja Michalska, Izaskun Buendia, Maria Luisa Jimeno, Daniel Jun, Jana Janockova, Vendula Sepsova, Ondrej Soukup, Oscar M Bautista-Aguilera, Bernard Refouvelet, Olivier Ouari, José Marco-Contelles, Lhassane Ismaili
Novel multifunctional tacrines for Alzheimer's disease were obtained by Ugi-reaction between ferulic (or lipoic acid), melatonin, formaldehyde, and tacrine derivatives, according to the antioxidant additive approach in order to modulate the oxidative stress as therapeutic strategy. Compound 5c has been identified as a promising permeable agent showing excellent antioxidant properties, strong cholinesterase inhibitory activity, less hepatotoxicity than tacrine, and the best neuroprotective capacity, being able to significantly activate the Nrf2 transcriptional pathway...
October 13, 2016: Journal of Medicinal Chemistry
Brenna M Flannery, Donald A Bruun, Douglas J Rowland, Christopher N Banks, Adam T Austin, David L Kukis, Yonggang Li, Byron D Ford, Daniel J Tancredi, Jill L Silverman, Simon R Cherry, Pamela J Lein
BACKGROUND: Acute intoxication with organophosphorus (OP) cholinesterase inhibitors can trigger convulsions that progress to life-threatening status epilepticus. Survivors face long-term morbidity including mild-to-severe decline in memory. It is posited that neuroinflammation plays a key role in the pathogenesis of OP-induced neuropsychiatric deficits. Rigorous testing of this hypothesis requires preclinical models that recapitulate relevant phenotypic outcomes. Here, we describe a rat model of acute intoxication with the OP diisopropylfluorophosphate (DFP) that exhibits persistent neuroinflammation and cognitive impairment...
October 12, 2016: Journal of Neuroinflammation
Pia Basaure, Fiona Peris-Sampedro, Maria Cabré, Ingrid Reverte, Maria Teresa Colomina
Cholinesterases (ChE) are common targets of organophosphate (OP) pesticides and play a critical role in the pathology of some dementias. While chlorpyrifos (CPF) remains one of the most commonly used OPs in the world, numerous investigations have reported its neurotoxic potential and highlighted behavioral disturbances upon its administration. Rivastigmine currently serves to treat Alzheimer's disease, but it may induce cholinergic overstimulation in non-demented individuals. The present investigation aimed to compare the acute and delayed effects caused by both ChE inhibitors in adult C57BL/6 male mice...
October 9, 2016: Behavioural Brain Research
Saeed Ahmad, Fariha Rashid Bhatti, Farhan Hameed Khaliq, Tehreem Younas, Asadullah Madni, Abida Latif
The present study demonstrates the biological study of Ficus carica fruit. Methanolic extract of plant fruit was prepared and evaporated under reduced pressure by rota vapor and n- hexane, Chloroform, ethyl acetate and n-butanol soluble fractions were prepared separately from crude methanolic extract. These fractions were then screened for acetyl cholinesterase, butryl cholinesterase and lipoxygenase activities. n-butanol soluble fraction showed significant antiacetylcholinesterase activity (78.55±0.76%) with IC50 of 55...
September 2016: Pakistan Journal of Pharmaceutical Sciences
Amanpreet Singh, Pushap Raj, Narinder Singh
The unregulated use of chemical weapons has aroused researchers to develop sensors for chemical warfare agents (CWA) and likewise to abolish their harmful effects, the degradation through catalysis has great advantage. Chemically, the CWAs are versatile; however, mostly they contain organophosphates that act on inhibition of acetyl cholinesterase. In this work, we have designed and synthesized some novel benzimidazolium based fluorescent cations and their fluorescent aggregates were fabricated using anionic surfactants (SDS and SDBS) in aqueous medium...
October 12, 2016: ACS Applied Materials & Interfaces
Gabriela Rodríguez-Fuentes, Valeria Marín-López, Esperanza Hernández-Márquez
Since several reports have indicated that cholinesterases (ChE) type and distribution is species specific and that in some species there is a relationship among gender, size and ChE activities, characterization has been suggested. The aim of the present study was to characterize the ChE present in head and muscle of Gambusia yucatana (using selective substrates and inhibitors) and to find its relationship with total length or gender. Results indicated that the ChE present in G. yucatana is an acetylcholinesterase (AChE) with high sensitivity to BW284C51 and an atypical smaller Km with butyrylthiocholine...
October 11, 2016: Bulletin of Environmental Contamination and Toxicology
Patrice Tremblay, Susan Gold
INTRODUCTION: Post-operative delirium (POD) is a serious surgical complication that can cause significant morbidity and mortality. It is associated with prolonged hospital stay, delayed admission to rehabilitation programs, persistent cognitive deficits, marked health-care costs, and more. The pathophysiology is multi-factorial and not completely understood, which complicates the optimal management. Non-pharmacological measures have been the mainstay of treatment, but there has been an ongoing interest in the medical literature on the prevention of post-operative delirium using medications...
September 2016: Canadian Geriatrics Journal: CGJ
Veeranna Gowda, Jayachandra, Raghavendra, Debasish Barik
No abstract text is available yet for this article.
January 2016: Journal of the Association of Physicians of India
Shaik Razia, Dilip M Rampure
No abstract text is available yet for this article.
January 2016: Journal of the Association of Physicians of India
Yingbo Fu, Yu Mu, Hui Lei, Pu Wang, Xin Li, Qiao Leng, Li Han, Xiaodan Qu, Zhanyou Wang, Xueshi Huang
Five novel tacrine-ferulic acid hybrid compounds (8a-e) were synthesized and their structures were identified on the basis of a detailed spectroscopic analysis. The activities of inhibiting acetyl cholinesterase (AChE) and butyryl cholinesterase (BuChE), reducing self-induced β-amyloid (Aβ) aggregation and chelating Cu(2+) were evaluated in vitro. Among them, 8c and 8d displayed the higher selectivity in inhibiting AChE over BuChE. Moreover, 8d also showed dramatic inhibition of self-Aβ aggregation, activity of chelating Cu(2+) and activity against Aβ-induced neurotoxicity in Neuro-2A cells...
October 11, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Sofía Otero, Gisela Kristoff
Organophosphate insecticides (OPs) continue to be an important class of agrochemicals used in modern agriculture worldwide. Even though these pesticides persist in the environment for a relatively short time, they show a high acute toxicity that may represent a serious hazard for wildlife. Sub-lethal effects on non-target species are a focus in pest management programs and should be used as biomarkers. Cholinesterases (ChEs) are the most used biomarker of OP exposure in vertebrate and invertebrate species. However, the combined monitoring of ChE and carboxylesterase (CE) activities may provide a more useful indication of exposure and effect of the organisms...
October 6, 2016: Aquatic Toxicology
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"