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https://www.readbyqxmd.com/read/29452304/the-chondrocyte-channelome-a-narrative-review
#1
Ali Mobasheri, Csaba Matta, Ilona Uzielienè, Emma Budd, Pablo Martín-Vasallo, Eiva Bernotiene
Chondrocytes are the main cells in the extracellular matrix of articular cartilage and possess a highly differentiated phenotype that is the hallmark of the unique physiological functions of this specialised load-bearing connective tissue. The plasma membrane of articular chondrocytes contains a rich and diverse complement of membrane proteins, known as the membranome, which defines the cell surface phenotype of the cells. The membranome is a key target of pharmacological agents and is important for chondrocyte function...
February 13, 2018: Joint, Bone, Spine: Revue du Rhumatisme
https://www.readbyqxmd.com/read/29452256/modulation-of-oxidative-stress-response-by-flaxseed-oil-role-of-lipid-peroxidation-and-underlying-mechanisms
#2
REVIEW
Rajnish Kumar Yadav, Manjari Singh, Subhadeep Roy, Mohd Nazam Ansari, Abdulaziz S Saeedan, Gaurav Kaithwas
Polyunsaturated fatty acids (PUFA's) are majorly classified as ω-3 and ω-6 fatty acids. The eicosapentaenoic acid (EPA, ω-3:20-5), docosahexaenoic acid (DHA, ω-3:22-6) and alpha-linolenic acid (ALA, ω-3:18-3) are known ω-3 fatty acids, extracted from animal (e.g fish oil) and plant sources (e.g flaxseed oil). Furthermore, linoleic acid (LA, ω-6:18-2) is recognized as ω-6 fatty acid and the most prominent biological fatty acid with a pro-inflammatory response. Flaxseed oil has variety of biological roles, due to a significant amount of ω-3/ω-6 fatty acids...
February 13, 2018: Prostaglandins & Other Lipid Mediators
https://www.readbyqxmd.com/read/29452207/glycogen-synthase-kinase-3%C3%AE-promotes-liver-innate-immune-activation-by-restraining-amp-activated-protein-kinase-activation
#3
Haoming Zhou, Han Wang, Ming Ni, Shi Yue, Yongxiang Xia, Ronald W Busuttil, Jerzy W Kupiec-Weglinski, Ling Lu, Xuehao Wang, Yuan Zhai
BACKGROUND & AIMS: Glycogen synthase kinase 3β (Gsk3β) is a ubiquitously expressed kinase with distinctive functions in different types of cells. Although its roles in regulating innate immune activation and ischemia and reperfusion injuries (IRI) have been well documented, underlying mechanisms remain ambiguous, due in part to the lack of cell-specific tools in vivo. METHODS: We created a myeloid-specific Gsk3β KO strain to study its function in macrophages in a murine liver partial warm ischemia model...
February 13, 2018: Journal of Hepatology
https://www.readbyqxmd.com/read/29452186/lectin-obtained-from-the-red-seaweed-bryothamnion-triquetrum-secondary-structure-and-anti-inflammatory-activity-in-mice
#4
Thais Pontes Carvalho Fontenelle, Glauber Cruz Lima, Jacilane Ximenes Mesquita, José Luiz de Souza Lopes, Tarcísio Vieira de Brito, Francisco das Chagas Vieira Júnior, Adriano Bezerra Sales, Karoline Saboia Aragão, Marcellus Henrique Loiola Ponte Souza, André Luiz Dos Reis Barbosa, Ana Lúcia Ponte Freitas
Seaweeds are sources of biomolecules with biological activities and pharmacological potential - for example, lectins, a group of proteins that can bind reversibly to carbohydrates or compounds containing them. The aim of this study was to elucidate the structural properties of a lectin extracted from the red seaweed Bryothamnion triquetrum (BtL) and to investigate its anti-inflammatory activity in mice. The lectin was purified by precipitation with ammonium sulfate and ion-exchange chromatography. Its secondary structure and tryptophan (Trp) microenvironment were analyzed by circular dichroism spectroscopy and steady-state fluorescence spectroscopy, respectively...
February 13, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29452181/the-demosponge-pseudoceratina-purpurea-as-a-new-source-of-fibrous-chitin
#5
Sonia Żółtowska-Aksamitowska, Mikhail Tsurkan, Swee-Cheng Lim, Heike Meissner, Konstantin Tabachnick, Lamiaa A Shaala, Diaa T A Youssef, Viatcheslav N Ivanenko, Iaroslav Petrenko, Marcin Wysokowski, Nicole Bechmann, Yvonne Joseph, Teofil Jesionowski, Hermann Ehrlich
Among marine demosponges (Porifera: Demospongiae), only representatives of the order Verongiida have been recognized to synthetize both biologically active substances as well as scaffolds-like fibrous skeletons made of structural aminopolysaccharide chitin. The unique 3D architecture of such scaffolds open perspectives for their applications in waste treatment, biomimetics and tissue engineering. Here, we focus special attention to the demosponge Pseudoceratina purpurea collected in the coastal waters of Singapore...
February 13, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29452148/complete-inhibition-of-fetal-movement-in-the-day-40-pregnant-goat-model-by-the-piperidine-alkaloid-anabasine-but-not-related-alkaloids
#6
B T Green, S T Lee, J W Keele, K D Welch, D Cook, J A Pfister, W R Kem
Four chemically similar alkaloids, anabasine, anabaseine, epibatidine and dimethylphenylpiperazinium (DMPP), are potent nicotinic acetylcholine receptor agonists of fetal muscle nicotinic acetylcholine receptors in human TE-671 cells. Based on results with these cells, we hypothesized that the alkaloids would completely inhibit ultrasound-monitored fetal movement in a goat model. Different, single doses of anabasine, anabaseine, epibatidine, DMPP, or saline control were administered I.V. to pregnant goats on day 40 of gestation and the number of fetal movements per 5 min sample was measured by ultrasound at times 0, 0...
February 13, 2018: Toxicon: Official Journal of the International Society on Toxinology
https://www.readbyqxmd.com/read/29452141/a-rich-source-of-potential-bioactive-compounds-with-anticancer-activities-by-catharanthus-roseus-cambium-meristematic-stem-cell-cultures
#7
So Hyun Moon, Muthuraman Pandurangan, Doo Hwan Kim, Jelli Venkatesh, Rahul V Patel, Bhupendra M Mistry
ETHNOPHARMACOLOGICAL IMPORTANCE: Catharanthus roseus (L.) G. Don. is an important medicinal plant with rich sources of remarkable health benefits consisting more than 100 alkaloids and significant amounts of bioactive compounds, which have been widely used as a folk medicine for treatment of several pathologies. THE AIM OF THE STUDY: In the present study, we isolated and cultured innately undifferentiated cambium meristematic cells (CMCs), which were observed stable cell growth, enhancement of bioactive compounds from C...
February 13, 2018: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29451997/poly-lactic-co-glycolic-acid-as-a-slow-release-drug-carrying-matrix-for-methotrexate-coated-onto-intraocular-lenses-to-conquer-posterior-capsule-opacification
#8
Stefan A Kassumeh, Christian M Wertheimer, Annabel von Studnitz, Anna Hillenmayer, Claudia Priglinger, Armin Wolf, Wolfgang J Mayer, Daniel Teupser, Lesca M Holdt, Siegfried G Priglinger, Kirsten H Eibl-Lindner
PURPOSE: Posterior capsule opacification (PCO) still represents the main long-term complication of cataract surgery. Research into pharmacologic PCO prophylaxis is extensive. One promising candidate drug is methotrexate (MTX). Our aim is to determine the in vitro feasibility of MTX-loaded poly(lactic-co-glycolic) (PLGA) biomatrices sprayed on intraocular lenses (IOLs) as a drug-delivery implant. METHODS: Hydrophilic and hydrophobic acrylic IOLs were spray-coated with MTX-loaded PLGA...
February 16, 2018: Current Eye Research
https://www.readbyqxmd.com/read/29451932/in-vitro-screening-of-the-antibacterial-and-anti-candida-properties-of-crushed-nonantimicrobial-drugs-frequently-prescribed-in-nursing-homes
#9
Julie Lamure, Marlène Chevalier, Pascal Rathelot, Françoise Mignolet, Isabelle Precheur
Frail older adults often experience swallowing disorders, prompting nursing staff to crush tablets, open capsules, and mix drugs into their meals or gelled water. However, crushing drugs can lead to pharmacological and gustatory problems. As crushed drugs can stay in prolonged contact with oral microbial biofilm, the current study aimed to investigate their antimicrobial properties. Crushed drugs were diluted in 1 mL of isotonic water and assayed in vitro for: (a) growth inhibition of five bacterial strains and Candida albicans by the diffusion method; (b) inhibition of Streptococcus salivarius and C...
February 13, 2018: Research in Gerontological Nursing
https://www.readbyqxmd.com/read/29451821/protection-from-vascular-dysfunction-in-female-rats-with-chronic-stress-and-depressive-symptoms
#10
Steven D Brooks, Stan Hileman, Paul D Chantler, Samantha Milde, Kent C Lemaster, Stephanie Frisbee, J Kevin Shoemaker, Dwayne N Jackson, Jefferson C Frisbee
The increasing prevalence and severity of clinical depression is strongly correlated with vascular disease risk, creating a comorbid condition with poor outcomes, although demonstrating a sexual disparity where females are at lower risk than males for subsequent cardiovascular events. To determine potential mechanisms responsible for this protection against stress/depression-induced vasculopathy in females, we exposed male and female ({plus minus}ovariectomy) rats to the unpredictable chronic mild stress (UCMS) model for 8 weeks and determined depressive symptom severity, vascular reactivity in aortic rings (AR) and ex vivo middle cerebral arteries (MCA), and determined the profile of major metabolites regulating vascular tone...
February 16, 2018: American Journal of Physiology. Heart and Circulatory Physiology
https://www.readbyqxmd.com/read/29451813/modulatory-effects-of-alkaloid-extract-from-gongronema-latifolium-utazi-and-lasianthera-africana-editan-on-activities-of-enzymes-relevant-to-neurodegeneration
#11
Esther E Nwanna, Adeniyi A Adebayo, Ganiyu Oboh, Opeyemi B Ogunsuyi, Ayokunle O Ademosun
Most alkaloids are produced by plants as a defense mechanism against herbivores. Since alkaloids are known to possess pharmacological effects, this study sought to investigate the in vitro modulatory effect of alkaloid obtained from two commonly consumed vegetables in southern Nigeria, Lasianthera africana (editan) and Gongronema latifolium (utazi), on some enzyme activities relevant to neurodegeneration. Effects of the alkaloids on cholinesterases (acetylcholinesterase [AChE] and butyrylcholinesterase [BChE]) and monoamine oxidase (MAO) activities were determined in vitro...
February 16, 2018: Journal of Dietary Supplements
https://www.readbyqxmd.com/read/29451744/design-synthesis-and-biological-evaluation-of-novel-bivalent-ligands-targeting-dopamine-d2-like-receptors-and-%C3%A2%C2%B5-opioid-receptor
#12
Mingcheng Qian, Lakshmi Vasudevan, Jelle Huysentruyt, Martijn D P Risseeuw, Christophe Stove, Patrick M L Vanderheyden, Kathleen Van Craenenbroeck, Serge Van Calenbergh
Nowadays, there is mounting evidence that intermolecular receptor-receptor interactions may result in altered receptor recognition, pharmacology and signaling. Heterobivalent ligands have been proven useful molecular probes for confirming and targeting heteromeric receptors. This paper describes the design and synthesis of novel heterobivalent ligands for dopamine D2-like receptors (D2-likeR) and the µ opioid receptor (µOR) and their evaluation using radioactive ligand binding and functional assays.
February 16, 2018: ChemMedChem
https://www.readbyqxmd.com/read/29451703/mechanisms-of-imidazoline-i-2-receptor-agonist-induced-antinociception-in-rats-involvement-of-monoaminergic-neurotransmission
#13
Justin N Siemian, Kaixuan Wang, Yanan Zhang, Jun-Xu Li
BACKGROUND AND PURPOSE: Although studies have established the antinociceptive efficacies of imidazoline I 2 receptor (I 2 R) agonists, its exact post-receptor mechanism remains unknown. This study tested the hypothesis that monoaminergic transmission is critical for I 2 R agonist-induced antinociception. EXPERIMENTAL APPROACH: The von Frey filament test was used to examine the antinociceptive effects of the I 2 R agonists 2-BFI and CR4056 on chronic constriction injury (CCI)-induced neuropathic pain or complete Freund's adjuvant (CFA)-induced inflammatory pain in rats...
February 16, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29451687/gpcrs-in-context-sexual-dimorphism-in-the-cardiovascular-system
#14
REVIEW
Margaret A Mouat, James L J Coleman, Nicola J Smith
Cardiovascular disease remains the largest cause of mortality worldwide and there is a clear gender gap in disease occurrence: men are predisposed to earlier onset of cardiovascular disease, including atherosclerosis and hypertension, than are women. Oestrogen may be a driving factor for female-specific cardioprotection, though androgens and sex chromosomes are also likely to contribute to sexual dimorphism in the cardiovascular system. Many G protein-coupled receptor (GPCR)-mediated processes are involved in cardiovascular homeostasis and some exhibit clear sex-divergence...
February 16, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29451686/an-iminium-ion-metabolite-hampers-the-production-of-the-pharmacologically-active-metabolite-of-a-multikinase-inhibitor-kw-2449-in-primates-irreversible-inhibition-of-aldehyde-oxidase-and-covalent-binding-with-endogenous-proteins
#15
Jun Hosogi, Rui Ohashi, Hiroshi Maeda, Kazuhiro Fujita, Junko Ushiki, Takashi Kuwabara, Yorihiro Yamamoto, Toru Imamura
We previously reported that KW-2449, (E)-1-{4-[2-(1H-Indazol-3-yl)vinyl]benzoyl}piperazine, a novel multikinase inhibitor developed for the treatment of leukemia patients, was oxidized to an iminium ion intermediate by monoamine oxidase B (MAO-B) and then converted to its oxo-piperazine form (M1) by aldehyde oxidase (AO). However, we found that the significant decrease in the pharmacologically active metabolite M1 following repeated administration of KW-2449 in primates might hamper the effectiveness of the drug...
February 16, 2018: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/29451665/mirror-therapy-a-potential-intervention-for-pain-management
#16
Priscilla G Wittkopf, Mark I Johnson
The consequences of chronic pain and associated disabilities to the patient and to the health care system are well known. Medication is often the first treatment of choice for chronic pain, although side effects and high costs restrict long-term use. Inexpensive, safe and easy to self-administer non-pharmacological therapies, such as mirror therapy, are recommended as adjuncts to pain treatment. The purpose of this review is to describe the principles of use of mirror therapy so it can be incorporated into a health care delivery...
November 2017: Revista da Associação Médica Brasileira
https://www.readbyqxmd.com/read/29451520/-hepatitis-c-virus-infection-from-clinical-guidelines-to-clinical-practice-and-personalization-of-cure
#17
Pierluigi Toniutto
Although clinical guidelines provide clear indications on the treatment of patients with chronic HCV related liver disease, there are still clinical situations in which clinicians experience and judgment remain essential in the proper patient management. These are mainly represented by antiviral therapy in patients with decompensated liver disease, especially if they are candidates for liver transplantation or with significant comorbidities and complex pharmacological therapies. Antiviral retreatment of patients who failed a regimen containing an NS5A protease inhibitor still appears to be a delicate context in which no solid recommendations are provided, especially in patients with HCV genotype 3 and decompensated cirrhosis...
January 2018: Recenti Progressi in Medicina
https://www.readbyqxmd.com/read/29451470/use-of-integrated-clinical-trial-protocols-a-survey-in-early-medicines-development
#18
Katharina Erb-Zohar, Hildegard Sourgens, Kerstin Breithaupt-Groegler
PURPOSE: To collect information on the use of integrated protocols in early clinical medicines development. MATERIALS AND METHODS: The questionnaire was mailed in fall 2014 to members of human pharmacology societies in Europe for anonymous responses via the online tool SurveyMonkey®. RESULTS: 97 respondents reported on 164 integrated protocols overall. In general, integrated protocols comprised 2 or 3 trial elements. One third of integrated protocols involved patients...
February 16, 2018: International Journal of Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29451407/advancements-in-drug-development-for-diarrhea-predominant-irritable-bowel-syndrome
#19
Giovanni Dothel, Maria Raffaell Barbaro, Emanuel Raschi, Giovanni Barbara, Fabrizio De Ponti
Introduction Diarrhea-predominant irritable bowel syndrome (IBS-D) is a common disorder characterized by a complex pathophysiology hampering optimal targeted drug development. Recent advances in our understanding of key underlying mechanisms prompted novel therapeutics including novel pharmacological approaches. Areas covered This review summarizes the latest advancements in the pipeline of IBS-D drugs focusing on new pharmacological targets, efficacy and safety of medicinal products considering the recent harmonization of regulatory requirements by the FDA and the EMA...
February 16, 2018: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/29451400/designing-selective-modulators-for-the-nicotinic-receptor-subtypes-challenges-and-opportunities
#20
Dina Manetti, Cristina Bellucci, Niccolò Chiaramonte, Silvia Dei, Elisabetta Teodori, Maria Novella Romanelli
Nicotinic receptors are membrane proteins involved in several physiological processes. They are considered suitable drug targets for various CNS disorders or conditions, as shown by the large number of compounds which have entered clinical trials. In recent years, nonconventional agonists have been discovered: positive allosteric modulators, allosteric agonists, site-specific agonists and silent desensitizers are compounds able to modulate the receptor interacting at sites different from the orthodox one, or to desensitize the receptor without prior opening...
February 16, 2018: Future Medicinal Chemistry
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