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https://www.readbyqxmd.com/read/29793211/synthesis-and-evaluation-of-novel-triazolyl-quinoline-derivatives-as-potential-antileishmanial-agents
#1
Akanksha Upadhyay, Pragati Kushwaha, Sampa Gupta, Ranga Prasad Dodda, Karthik Ramalingam, Ruchir Kant, Neena Goyal, Koneni V Sashidhara
The high potential of quinoline containing natural products and their derivatives in medicinal chemistry led us to discover novel series of 25 compounds for the development of new antileishmanial agents. A series of triazolyl 2-methyl-4-phenylquinoline-3-carboxylate derivatives has been synthesized via click chemistry inspired molecular hybridization approach and evaluated against Leishmania donovani. Most of the screened derivatives exhibited significant in vitro anti-leishmanial activity against promastigote (IC50 ranging from 2...
May 12, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29793179/nano-strategies-for-berberine-delivery-a-natural-alkaloid-of-berberis
#2
REVIEW
Elaheh Mirhadi, Mehdi Rezaee, Bizhan Malaekeh-Nikouei
Berberine, as a phytochemical component of some medicinal Chinese herbs (most frequently Berberis vulgaris), is an isoquinoline alkaloid with many therapeutic effects including anti-viral, anti-microbial, anti-diarrhea, anti-inflammatory and anti-tumor effects. Berberine has some significant effects on type 2 diabetes through adenosine monophosphate-activated protein kinase activation, glycolysis stimulation, and mitochondrial function inhibition which subsequently improves both lipid and glucose metabolism...
May 21, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29793142/synthesis-of-aryl-pyrazole-via-suzuki-coupling-reaction-in-vitro-mushroom-tyrosinase-enzyme-inhibition-assay-and-in-silico-comparative-molecular-docking-analysis-with-kojic-acid
#3
Pervaiz Ali Channar, Aamer Saeed, Fayaz Ali Larik, Bakhtawar Batool, Saima Kalsoom, M M Hasan, Mauricio F Erben, Hesham R El-Seedi, Musrat Ali, Zaman Ashraf
Aryl pyrazoles are well recognized class of heterocyclic compounds found in several commercially available drugs. Owing to their significance in medicinal chemistry, in this current account we have synthesized a series of suitably substituted aryl pyrazole by employing Suzuki cross-coupling reaction. All compounds were evaluated for inhibition of mushroom tyrosinase enzyme both in vitro and in silico. Compound 3f (IC50  = 1.568 ± 0.01 µM) showed relatively better potential compared to reference kojic acid (IC50  = 16...
April 30, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29793137/3-o-sulfation-of-heparin-leads-to-hepatotropism-and-longer-circulatory-half-life
#4
Colton M Miller, Yongmei Xu, Katrina M Kudrna, Blake E Hass, Brianna M Kellar, Andrew W Egger, Jian Liu, Edward N Harris
INTRODUCTION: Heparins are common blood anticoagulants that are critical for many surgical and biomedical procedures used in modern medicine. In contrast to natural heparin derived from porcine gut mucosa, synthetic heparins are homogenous by mass, polymer length, and chemistry. MATERIALS & METHODS: Stable cell lines expressing the human and mouse Stabilin receptors were used to evaluate endocytosis of natural and synthetic heparin. We chemoenzymatically produced synthetic heparin consisting of 12 sugars (dodecamers) containing 14 sulfate groups resulting in a non-3-O sulfated structure (n12mer)...
May 17, 2018: Thrombosis Research
https://www.readbyqxmd.com/read/29793124/how-to-manage-patellofemoral-pain-understanding-the-multifactorial-nature-and-treatment-options
#5
Simon Lack, Bradley Neal, Danilo De Oliveira Silva, Christian Barton
Patellofemoral pain (PFP) is one of the most prevalent conditions within sports medicine, orthopaedic and general practice settings. Long-term treatment outcomes are poor, with estimates that more than 50% of people with the condition will report symptoms beyond 5 years following diagnosis. Additionally, emerging evidence indicates that PFP may be on a continuum with patellofemoral osteoarthritis. Consensus of world leading clinicians and academics highlights the potential benefit of delivering tailored interventions, specific to an individual's needs, to improve patient outcome...
April 12, 2018: Physical Therapy in Sport
https://www.readbyqxmd.com/read/29793085/socio-demographic-factors-associated-with-choosing-violent-methods-of-suicide-2011-2016-ilam-province
#6
Yousef Veisani, Fathola Mohamadian, Ali Delpisheh, Salman Khazaei
BACKGROUND: In new strategies towards of suicide prevention the best approach currently is based on specific method had specific risk factors. Therefore in this study we aimed to find out the association between socio-demographic factors and methods in completed suicide, 2011-2016, Ilam province. METHODS: A cross-sectional study, 2011-2016, was conducted. A total of 540 completed suicides were recruited to the study. Data were collected by systematic registration suicide data (SRSD) and Legal Medicine Organization (LMO)...
May 21, 2018: Asian Journal of Psychiatry
https://www.readbyqxmd.com/read/29792985/novel-excipients-regulatory-challenges-and-perspectives-the-eu-insight
#7
Piotr Kozarewicz, Thorsteinn Loftsson
Novel excipients are indispensable in development of modern, advanced drug delivery systems and biotechnology-derived drugs. Although numerous novel excipients are developed for pharmaceutical use, they are not frequently seen in medicinal products due to the strict regulatory requirements and perception that their use makes new product evaluation more complex with risk of delays in the approval process. Regulators regard novel excipients as new substances and whenever new excipient is used in a formulation it must be subjected to full evaluation, similarly to the one required for new active substance...
May 21, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29792980/language-used-by-health-care-professionals-to-describe-dying-at-an-acute-care-hospital
#8
Kirsten Wentlandt, Philippe Toupin, Natalia Novosedlik, Lisa W Le, Camilla Zimmermann, Ebru Kaya
PURPOSE: To understand the language used to describe the deterioration and death of patients in an acute academic tertiary care centre, and to identify whether patient diagnoses or palliative care(PC) involvement was associated with clearer descriptions of this process. METHODS: We conducted a retrospective chart review of the final admission of 150 patients who died on an inpatient internal medicine unit. Conventional and summative content analysis was performed of the language used to describe, either directly or indirectly, that the patient's death was imminent...
May 21, 2018: Journal of Pain and Symptom Management
https://www.readbyqxmd.com/read/29792967/validated-reverse-phase-hplc-diode-array-method-for-the-quantification-of-intact-bevacizumab-infliximab-and-trastuzumab-for-long-term-stability-study
#9
Antonio Martínez-Ortega, Agustín Herrera, Antonio Salmerón-García, José Cabeza, Luis Cuadros-Rodríguez, Natalia Navas
The aim of the present study was to develop suitable and reliable method for quantification three of the most worldwide used therapeutic monoclonal antibodies (mAbs) -bevazizumab (BVZ), infliximab (INF) and trastuzumab (TTZ)- to be used in long-term stability studies. Reverse phase (RP) was selected by its greater sensibility and reproducibility comparing with other chromatographic modes. Then a high performance liquid chromatography with diode array detection (RP)HPLC/DAD method was checked. Since the three mAbs represent the active ingredient in the medicines in which they are formulated, the selected method was validated for each one in accordance with the International Conference on Harmonization (ICH) guidelines for pharmaceuticals for human use...
May 21, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29792965/characterization-sulfated-modification-and-bioactivity-of-a-novel-polysaccharide-from-millettia-dielsiana
#10
Zhonghua Wang, Tongqiang Cai, Xipu He
Millettia dielsiana is a traditional herb medicine to treat rheumatic arthritis and gynecological diseases. In this study, a novel polysaccharide (MDP1) with a molecular weight of 139.54 kDa was isolated from Millettia dielsiana by DEAE-52 cellulose chromatography. Its sulfated derivative (S-MDP1) was prepared by the chlorosulfonic acid-pyridine method. Structural analysis indicated that MDP1 was a pectic polysaccharide and did not exhibit a triple helical conformation. In vitro, MDP1 and S-MDP1 had protective effect on H2 O2 -induced PC12 cells death...
May 21, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29792959/fabrication-and-cytotoxicity-assessment-of-cellulose-nanofibrils-using-bassia-eriophora-biomass
#11
Jegan Athinarayanan, Vaiyapuri Subbarayan Periasamy, Ali A Alshatwi
Cellulose nanofibrils (CNs) are eco-friendly, biodegradable, biocompatible, renewable, cost-effective, and possess excellent mechanical properties. We fabricated CNs from Bassia eriophora biomass, and the structure and morphology were investigated by transmission electron microscopy that revealed 2-6 μm long fibrillated structures with diameters of 15-40 nm. CNs biocompatibility was assessed using in vitro based assays, including cell viability assay, AO/EB staining, Hoechst staining, JC-1 staining, and gene expression analysis...
May 21, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29792919/seeing-the-light-shifting-from-wild-rhizomes-to-extraction-of-active-ingredients-from-above-ground-parts-of-paris-polyphylla-var-yunnanensis
#12
Xu-Jie Qin, Wei Ni, Chang-Xiang Chen, Hai-Yang Liu
ETHNOPHARMACOLOGICAL RELEVANCE: The dried rhizomes of Paris polyphylla var. yunnanensis are widely used in traditional Chinese medicine (TCM) as hemostatic, antitumor, and antimicrobial agents. More than 70 Chinese patent medicines are based on P. polyphylla var. yunnanensis rhizomes. Steroidal saponins are considered as the main active ingredients of these rhizomes. However, wild populations of P. polyphylla var. yunnanensis are greatly threatened due to the illegal wild harvest and over-utilization of the rhizomes...
May 21, 2018: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29792918/translational-omics-future-potential-and-current-challenges-in-precision-medicine
#13
Arsalan Wafi, Reza Mirnezami
Rapid advances in computational science and biotechnology are paving the way for precision medicine - a vision in next-generation healthcare that promises to provide a care package uniquely tailored to each individual's molecular make-up. Until relatively recently, the focus has been firmly centred around the genome; however, over the past two decades there has been a surge in the study of molecular activity within other biological domains (proteome/transcriptome/metabolome) involved in health and pathogenesis...
May 21, 2018: Methods: a Companion to Methods in Enzymology
https://www.readbyqxmd.com/read/29792906/four-novel-antibacterial-sesquiterpene-%C3%AE-amino-acid-quaternary-ammonium-hybrids-from-the-mycelium-of-mushroom-stereum-hirsutum
#14
Yuan-Chang Duan, Jun Feng, Na Bai, Guo-Hong Li, Ke-Qin Zhang, Pei-Ji Zhao
The mushroom Stereum hirsutum is parasitized by Tremella aurantia to form a heterogeneous basidiocarp Jin'er, which has been used as food and folk medicine in Chinese society. In present work, the S. hirsutum was fermented in YMG broth, and four novel mixed terpenes, stereumamides A-D (1-4), which are sesquiterpenes combined with α-amino acids to form quaternary ammonium hybrids, were isolated from the Stereum hirsutum FP-91666 and their structures were elucidated by spectroscopic data analysis. Stereumamides A and D showed antibacterial activity against Escherichia coli, Staphylococcus aureus, and Salmonella typhimurium, with the minimum inhibitory concentration (MIC) values of 12...
May 21, 2018: Fitoterapia
https://www.readbyqxmd.com/read/29792873/effect-of-alzheimer-s-disease-risk-and-protective-factors-on-cognitive-trajectories-in-subjective-memory-complainers
#15
Stefan J Teipel, Enrica Cavedo, Simone Lista, Marie-Odile Habert, Marie-Claude Potier, Michel J Grothe, Stephane Epelbaum, Luisa Sambati, Geoffroy Gagliardi, Nicola Toschi, Michael Greicius, Bruno Dubois, Harald Hampel
INTRODUCTION: Cognitive change in people at risk of Alzheimer's disease (AD) such as subjective memory complainers is highly variable across individuals. METHODS: We used latent class growth modeling to identify distinct classes of nonlinear trajectories of cognitive change over 2 years follow-up from 265 subjective memory complainers individuals (age 70 years and older) of the INSIGHT-preAD cohort. We determined the effect of cortical amyloid load, hippocampus and basal forebrain volumes, and education on the cognitive trajectory classes...
May 21, 2018: Alzheimer's & Dementia: the Journal of the Alzheimer's Association
https://www.readbyqxmd.com/read/29792820/hydrogel-tissue-chemistry-principles-and-applications
#16
Viviana Gradinaru, Jennifer Treweek, Kristin Overton, Karl Deisseroth
Over the past five years, a rapidly developing experimental approach has enabled high-resolution and high-content information retrieval from intact multicellular animal (metazoan) systems. New chemical and physical forms are created in the hydrogel-tissue chemistry process, and the retention and retrieval of crucial phenotypic information regarding constituent cells and molecules (and their joint interrelationships) are thereby enabled. For example, rich data sets defining both single-cell-resolution gene expression and single-cell-resolution activity during behavior can now be collected while still preserving information on three-dimensional positioning and/or brain-wide wiring of those very same neurons-even within vertebrate brains...
May 20, 2018: Annual Review of Biophysics
https://www.readbyqxmd.com/read/29792780/cardiovascular-screening-practices-and-attitudes-from-the-ncaa-autonomous-power-5-conferences
#17
Christopher W Miars, Andreas Stamatis, Grant B Morgan, Jonathan A Drezner
BACKGROUND: The development of athlete-specific electrocardiogram (ECG) interpretation standards, along with recent rates of sudden cardiac death (SCD) in athletes being higher than previously estimated, has heightened the debate in the sports medicine community regarding cardiovascular screening of the college athlete, including whether certain high-risk subsets, such as male basketball athletes, should undergo more intensive screening. HYPOTHESIS: ECG and/or echocardiography screening in National Collegiate Athletic Association Autonomous 5 Division I (A5DI) schools will be more common than previous reports, and there will be more frequent use of noninvasive cardiac screening for men's basketball players than the general athlete population...
May 1, 2018: Sports Health
https://www.readbyqxmd.com/read/29792727/added-value-of-including-entire-brain-on-body-imaging-with-fdg-pet-mri
#18
Ana M Franceschi, Robert Matthews, Lev Bangiyev, Nand Relan, Ammar Chaudhry, Dinko Franceschi
OBJECTIVE: FDG PET/MRI examination of the body is routinely performed from the skull base to the mid thigh. Many types of brain abnormalities potentially could be detected on PET/MRI if the head was included. The objective of this study was therefore to identify and characterize brain findings incidentally detected on PET/MRI of the body with the head included. MATERIALS AND METHODS: We retrospectively identified 269 patients with FDG PET/MRI whole-body scans that included the head...
May 24, 2018: AJR. American Journal of Roentgenology
https://www.readbyqxmd.com/read/29792723/-experimental-promotion-of-liver-regeneration-after-portal-vein-branch-ligation
#19
V Liška, V Třeška, H Mírka, O Vyčítal, J Brůha, L Haidingerová, J Beneš, Z Tonar, R Pálek, J Rosendorf
INTRODUCTION: Portal vein embolization or ligation (PVE/PVL) is part of most multi-stage liver procedures in the case of low future liver remnant volume (FLRV). PVE initiates compensatory hypertrophy of non-occluded liver parenchyma. This hypertrophy is stimulated by an increased volume of portal blood in the non-occluded veins. PVE results in adequate FLRV growth necessary for resection only in 63-96% patients. The aim of this publication is to summarize the possibilities of influencing liver regeneration after PVE/PVL in an experiment using cytokines (TNF-α, IL-6), a monoclonal antibody against TGF-β1 (MAB TGF-β1) and mesenchymal stem cells (MSC)...
2018: Rozhledy V Chirurgii: Měsíčník Československé Chirurgické Společnosti
https://www.readbyqxmd.com/read/29792720/-experimental-processing-of-corrosion-casts-of-large-animal-organs
#20
R Pálek, V Liška, L Eberlová, H Mírka, M Svoboda, S Haviar, M Emingr, O Brzoň, P Mik, V Třeška
INTRODUCTION: Corrosion casts (CCs) are used for the visualization and assessment of hollow structures. CCs with filled capillaries enable (with the help of imaging methods) to obtain data for mathematical organ perfusion modelling. As the processing is more difficult in case of organs with greater volume of the vasculature, mainly organs from small animals have been cast up to now. The aim of this study was to optimize the protocol of corrosion casting of different organs of pig. Porcine organs are relatively easily accessible and frequently used in experimental medicine...
2018: Rozhledy V Chirurgii: Měsíčník Československé Chirurgické Společnosti
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