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https://read.qxmd.com/read/30776373/signaling-characteristics-and-functional-regulation-of-delta-opioid-kappa-opioid-receptor-dop-kop-heteromers-in-peripheral-sensory-neurons
#1
Blaine A Jacobs, Miryam M Pando, Elaine M Jennings, Raehannah J Jamshidi, Joshua C Zamora, Teresa S Chavera, William P Clarke, Kelly A Berg
Receptor heteromers often display distinct pharmacological and functional properties compared to the individual receptor constituents. In this study, we compared the properties of the DOP-KOP heteromer agonist, 6'-guanidinonaltrindole (6'-GNTI), with agonists for DOP ([D-Pen2,5]-enkephalin [DPDPE]) and KOP (U50488) in peripheral sensory neurons in culture and in vivo. In primary cultures, all three agonists inhibited PGE2 -stimulated cAMP accumulation as well as activated extracellular signal-regulated kinase 1/2 (ERK) with similar efficacy...
February 15, 2019: Neuropharmacology
https://read.qxmd.com/read/30775939/sweeteners-modulate-bioactivity-of-endothelial-progenitor-cells-but-not-induce-detrimental-effects-both-on-inflammation-and-behavioural-changes
#2
Concetta Schiano, Vincenzo Grimaldi, Serena Boccella, Monica Iannotta, Alberto Zullo, Livio Luongo, Francesco Paolo Mancini, Sabatino Maione, Claudio Napoli
This study sought to determine the possible detrimental effects of several low- or non-caloric sweeteners on endothelial progenitor cells (EPCs), inflammation and behavioural changes in mice. C57BL/6 male mice received low and high dose of natural and artificial sweeteners for 4 weeks. EPCs, physical and biochemical variables, inflammation and behavioural changes were evaluated. A significant reduction of about 25% of EPCs was found when mice received a moderate amount of all sweeteners (p < .05). This reduction was more strongly significant when a double dose of glucose, aspartame, rebaudioside A and cyclamate (p < ...
February 18, 2019: International Journal of Food Sciences and Nutrition
https://read.qxmd.com/read/30774656/-terminalia-tomentosa-bark-ameliorates-inflammation-and-arthritis-in-carrageenan-induced-inflammatory-model-and-freund-s-adjuvant-induced-arthritis-model-in-rats
#3
Srinivasa Reddy Jitta, Prasanthi Daram, Karthik Gourishetti, C S Misra, Picheswara Rao Polu, Abhishek Shah, C S Shreedhara, Madhavan Nampoothiri, Richard Lobo
Terminalia tomentosa bark belongs to the family Combretaceae. The plant bark is astringent and useful in the treatment of ulcers, vata, fractures, hemorrhages, bronchitis, and diarrhea. Phytochemical investigation of T. tomentosa bark confirms the presence of flavonoids, polyphenols, and tannins. The plant has not been investigated for its anti-inflammatory and antiarthritic activity. The present study was undertaken to explore its possible anti-inflammatory and antiarthritic activity. Anti-inflammatory activity of alcoholic and aqueous extracts of the bark was assessed by in vivo methods...
2019: Journal of Toxicology
https://read.qxmd.com/read/30763598/evidence-for-the-involvement-of-opioid-and-cannabinoid-systems-in-the-peripheral-antinociception-mediated-by-resveratrol
#4
Cristina da Costa Oliveira, Marina Gomes Miranda E Castor, Camila Gomes Miranda E Castor, Ághata de França Costa, Renata Cristina Mendes Ferreira, Josiane Fernandes da Silva, Juliana Maria Navia Pelaez, Luciano Dos Santos Aggum Capettini, Virginia Soares Lemos, Igor Dimitri Gama Duarte, Andrea de Castro Perez, Sérgio Henrique Sousa Santos, Thiago Roberto Lima Romero
Despite all the development of modern medicine, around 100 compounds derived from natural products were undergoing clinical trials only at the end of 2013. Among these natural substances in clinical trials, we found the resveratrol (RES), a pharmacological multi-target drug. RES analgesic properties have been demonstrated, although the bases of these mechanisms have not been fully elucidated. The aim of this study was to evaluate the involvement of opioid and cannabinoid systems in RES-induced peripheral antinociception...
February 11, 2019: Toxicology and Applied Pharmacology
https://read.qxmd.com/read/30759831/development-of-a-mucoadhesive-and-in-situ-gelling-formulation-based-on-%C3%AE%C2%BA-carrageenan-for-application-on-oral-mucosa-and-esophagus-walls-i-a-functional-in-vitro-characterization
#5
Barbara Vigani, Angela Faccendini, Silvia Rossi, Giuseppina Sandri, Maria Cristina Bonferoni, Matteo Gentile, Franca Ferrari
Oral mucositis and esophagitis represent the most frequent and clinically significant complications of cytoreductive chemotherapy and radiotherapy, which severely compromise the patient quality of life. The local application of polymeric gels could protect the injured tissues, alleviating the most painful symptoms. The present work aims at developing in situ gelling formulations for the treatment of oral mucositis and esophagitis. To reach these targets, κ-carrageenan (κ-CG) was selected as a polymer having wound healing properties and able to gelify in the presence of saliva ions, while hydroxypropyl cellulose (HPC) was used to improve the mucoadhesive properties of the formulations...
February 12, 2019: Marine Drugs
https://read.qxmd.com/read/30747721/inhibitory-effect-of-iota-carrageenan-on-porcine-reproductive-and-respiratory-syndrome-virus-in-vitro
#6
Chunhe Guo, Zhenbang Zhu, Piao Yu, Xiaoxiao Zhang, Wenjuan Dong, Xiaoying Wang, Yaosheng Chen, Xiaohong Liu
BACKGROUND: Porcine reproductive and respiratory syndrome virus (PRRSV) is an economically important pathogen and causes significant economic losses to the swine industry worldwide each year. Current vaccination strategies do not effectively prevent and control the virus. Consequently, it is necessary to develop novel antiviral strategies. Carrageenan, extracted from marine red algae, exhibits anti-coagulant, anti-tumor, anti-virus and immunomodulatory activities. METHODS: We investigate the inhibitory effect of iota-carrageenan (CG) on PRRSV strain CH-1a via antiviral assay and viral binding, entry and release assays...
February 12, 2019: Antiviral Therapy
https://read.qxmd.com/read/30738866/similarity-and-dissimilarity-in-antinociceptive-effects-of-dipeptidyl-peptidase-4-inhibitors-diprotin-a-and-vildagliptin-in-rat-inflammatory-pain-models-following-spinal-administration
#7
Mihály Balogh, Bence Kálmán Varga, Dávid Árpád Karádi, Pál Riba, Zita Puskár, Márk Kozsurek, Mahmoud Al-Khrasani, Kornél Király
Dipeptidyl-peptidase 4 (DPP4) enzyme is involved in the degradation of many biologically active peptides including opioids. Its role in pain transmission is poorly elucidated. Recently we reported on the spinal antihyperalgesic effects of DPP4 inhibitors, Ile-Pro-Ile (Diprotin A) and vildagliptin in carrageenan-evoked acute inflammatory pain in rats. The present study investigated the effects of intrathecal (it.) diprotin A and vildagliptin in Complete Freund's Adjuvant- (CFA) and formalin induced pain in rats...
February 7, 2019: Brain Research Bulletin
https://read.qxmd.com/read/30738730/biosynthesis-of-%C3%AE-aminobutyrate-by-engineered-lactobacillus-brevis-cells-immobilized-in-gellan-gum-gel-beads
#8
Chang-Jiang Lyu, Lu Liu, Jun Huang, Wei-Rui Zhao, Sheng Hu, Le-He Mei, Shan-Jing Yao
γ-Aminobutyrate (GABA) is an important chemical in pharmaceutical field. The use of lactic acid bacteria as biocatalysts for the conversion of l-monosodium glutamate (MSG) into GABA opens interesting perspectives for the production of this functional compound. In this work, an engineered GABA high-producing strain Lactobacillus brevis GadAΔC14 was constructed by overexpressing a C-terminally truncated GadA mutant, which is active in expanded pH range. After comparison with agar and κ-carrageenan, gellan gum was selected as the optimal immobilization support, and the properties of L...
February 7, 2019: Journal of Bioscience and Bioengineering
https://read.qxmd.com/read/30738132/development-of-morin-hydroxypropyl-%C3%AE-cyclodextrin-inclusion-complex-enhancement-of-bioavailability-antihyperalgesic-and-anti-inflammatory-effects
#9
Bruno Dos Santos Lima, Caio de Alcântara Campos, Anna Clara Ramos da Silva Santos, Victória Caroline Nunes Santos, Gabriela das Graças Gomes Trindade, Saravanan Shanmugam, Erik Willyame Menezes Pereira, Ricardo Neves Marreto, Marcelo Cavalcante Duarte, Jackson Roberto Guedes da Silva Almeida, Jullyana de Souza Siqueira Quintans, Lucindo José Quintans, Adriano Antunes de Souza Araújo
Morin is a flavonoid has been reported with several pharmacological effects such as, antioxidant, anti-inflammatory, anticancer, antidiabetic, etc. However, morin has low solubility in water, which decreases the bioavailability and limits its clinical application. In this way, to improve the pharmaceutical properties, morin was complexed in hydroxypropyl-β-cyclodextrin (HP-β-CD) and its oral bioavailability and anti-inflammatory effects were evaluated. Initially, a phase solubility study was performed, which showed that HP-β-CD would be the better cyclodextrin for the formation of complexes with morin...
February 6, 2019: Food and Chemical Toxicology
https://read.qxmd.com/read/30736095/dietary-interventions-for-induction-and-maintenance-of-remission-in-inflammatory-bowel-disease
#10
REVIEW
Berkeley N Limketkai, Zipporah Iheozor-Ejiofor, Teuta Gjuladin-Hellon, Alyssa Parian, Laura E Matarese, Kelly Bracewell, John K MacDonald, Morris Gordon, Gerard E Mullin
BACKGROUND: Inflammatory bowel disease (IBD), comprised of Crohn's disease (CD) and ulcerative colitis (UC), is characterized by chronic mucosal inflammation, frequent hospitalizations, adverse health economics, and compromised quality of life. Diet has been hypothesised to influence IBD activity. OBJECTIVES: To evaluate the efficacy and safety of dietary interventions on IBD outcomes. SEARCH METHODS: We searched the Cochrane IBD Group Specialized Register, CENTRAL, MEDLINE, Embase, Web of Science, Clinicaltrials...
February 8, 2019: Cochrane Database of Systematic Reviews
https://read.qxmd.com/read/30735820/enhanced-transdermal-permeation-and-anti-inflammatory-potential-of-phospholipids-complex-loaded-matrix-film-of-umbelliferone-formulation-development-physico-chemical-and-functional-characterization
#11
Darshan R Telange, Shivendra B Nirgulkar, Milind J Umekar, Arun T Patil, Anil M Pethe, Nikhil R Bali
In the present study, umbelliferone - phospholipids complex - loaded matrix film (UPLC - MF) was developed with a goal of improving transdermal permeation and anti-inflammatory potential of umbelliferone (UMB). Umbelliferone - phospholipids complex (UPLC) was prepared using solvent evaporation method. UPLC-MF was prepared by simple and reproducible solvent casting method. Prepared UPLC and UPLC-MF were both physico-chemically characterized by Fourier transforms infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), powder x-ray diffraction (PXRD), proton nuclear magnetic resonance spectroscopy (1 H NMR), weight variation, thickness, tensile strength, folding endurance, % elongation, moisture content and uptake Functional characterization of UPLC and UPLC-MF was carried out by solubility analysis, in vitro dissolution, diffusion, and ex vivo permeation via dialysis and biological membrane...
February 5, 2019: European Journal of Pharmaceutical Sciences
https://read.qxmd.com/read/30733853/shepherd-s-purse-polyphenols-exert-its-anti-inflammatory-and-antioxidative-effects-associated-with-suppressing-mapk-and-nf-%C3%AE%C2%BA-b-pathways-and-heme-oxygenase-1-activation
#12
Jinming Peng, Tianyong Hu, Jin Li, Jing Du, Kerui Zhu, Baohui Cheng, Kaikai Li
Shepherd's purse ( Capsella bursa-pastoris (L.) Medik.), a wild herb as a traditional herbal medicine, has been proved with multiple healthy benefits. In this study, the chemical constituents of shepherd's purse were identified by UPLC-QTOF-MS/MS. The antioxidative and anti-inflammatory potential of shepherd's purse extract (SPE) were also investigated applying lipopolysaccharide- (LPS-) induced inflammation in RAW 264.7 macrophages and a carrageenan-induced mice paw edema model. Twenty-four chemical compounds were identified mainly including phenolic acids and flavonoids...
2019: Oxidative Medicine and Cellular Longevity
https://read.qxmd.com/read/30732762/hybrid-%C3%AE%C2%BA-carrageenan-based-polymers-showing-schizophrenic-lower-and-upper-critical-solution-temperatures-and-potassium-responsiveness
#13
L Loukotová, A Bogomolova, R Konefal, M Špírková, P Štěpánek, M Hrubý
Novel multiresponsive hybrid biocompatible systems of κ-carrageenan-graft-poly(2-isopropyl-2-oxazoline-co-2-butyl-2-oxazoline)s with unique combination of responsiveness to external stimuli were synthesized and studied. The polymer thermoresponsive behavior proved the existence of both lower and upper critical solution temperatures in aqueous milieu, forming gel at lower temperature, a solution at room temperature and cloudy nanophase-separated dispersion at elevated temperature. The limit temperatures can easily be adjusted by the polyoxazoline graft length and grafting density...
April 15, 2019: Carbohydrate Polymers
https://read.qxmd.com/read/30720378/design-of-a-liquid-nano-sized-drug-delivery-system-with-enhanced-solubility-of-rivaroxaban-for-venous-thromboembolism-management-in-paediatric-patients-and-emergency-cases
#14
Dalia M N Abouhussein, Dina Bahaa El Din Mahmoud, Ebtehal Mohammad F
The increasing incidence of venous thromboembolism in paediatric population has stimulated the development of liquid anticoagulant formulations. Thus our goal is to formulate a liquid formulation of poorly-water soluble anticoagulant, Rivaroxaban, for paediatric use and to assess the possibility of its intravenous administration in emergencies. Self-nanoemulsifying drug delivery systems (SNEDDS) were developed and characterized. SNEDDS constituents were estimated from the saturated solubility study followed by plotting the corresponding ternary phase diagrams to determine the best self-emulsified systems...
February 5, 2019: Journal of Liposome Research
https://read.qxmd.com/read/30716621/cox-1-cox-2-inhibition-assays-and-histopathological-study-of-the-new-designed-anti-inflammatory-agent-with-a-pyrazolopyrimidine-core
#15
Eman K A Abdelall, Phoebe F Lamie, Amira K M Ahmed, El-Shaymaa El-Nahass
Four pyrazolopyrimidine series were prepared with a substitution at position- 4 by Schiff base, triazole, oxadiazole and pyrazole moieties (7a-f, 8a,b, 9a-f, 10a,b and 13a,b), respectively. All the synthesized compounds were evaluated in vitro against COX-2 and in vivo against carrageenan-induced rat paw edema as anti-inflammatory agents. Regarding the anti-inflammatory activity (AI) compounds 7c, 7f, 8a, and 9a showed higher activity with respect to celecoxib. Compounds 9a, 7d, and 7f were closely selective to celecoxib...
January 22, 2019: Bioorganic Chemistry
https://read.qxmd.com/read/30714176/investigation-of-anti-inflammatory-nitric-oxide-donating-vasorelaxation-and-ulcerogenic-activities-of-1-3-diphenylprop-2-en-1-one-derivatives-in-animal-models
#16
Amol Sherikar, Rakesh Dhavale, Manish Bhatia
The main aim of this work is to find out novel chemical moieties with potent anti-inflammatory and vasorelaxant activities with reduced gastric toxicities. For fulfilling the above aim, here we investigated novel chalcones (1, 3-diphenylprop-2-en-1-one derivatives) with nitric oxide (NO) and hydrogen sulfide (H2 S) donating potency for anti-inflammatory activity by carrageenan-induced rat paw edema. These molecules then further evaluated for in-vitro NO-releasing potency and vasorelaxation effect on isolated adult goat aortic tissue...
February 3, 2019: Clinical and Experimental Pharmacology & Physiology
https://read.qxmd.com/read/30713279/design-and-synthesis-of-triazole-phthalimide-hybrids-with-anti-inflammatory-activity
#17
Shalom P de O Assis, Moara T da Silva, Filipe Torres da Silva, Mirella P Sant'Anna, Carolina M B de Albuquerque Tenório, Caroline F Brito Dos Santos, Caíque S M da Fonseca, Gustavo Seabra, Vera L M Lima, Ronaldo N de Oliveira
Phthalimido-alkyl-1H-1,2,3-triazole derivatives 3a-d and 4a-d were efficiently synthesized using 1,3-dipolar cycloaddition reaction. Anti-inflammatory activity and toxicity studies were performed. The results demonstrated that all the tested compounds reduced carrageenan-induced paw edema and indicated no lethality for toxicity against Artemia salina and acute toxicity in vivo (LD50 up to 1 g kg -1 ). Furthermore, the structure of phthalimide linked to phenyl group proved to be more active than the compounds containing benzothiazole moiety...
2019: Chemical & Pharmaceutical Bulletin
https://read.qxmd.com/read/30703495/evaluation-of-anti-nociceptive-and-anti-inflammatory-activities-of-the-methanol-extract-of-holigarna-caustica-dennst-oken-leaves
#18
Md Adnan, Md Nazim Uddin Chy, A T M Mostafa Kamal, James W Barlow, Mohammad Omar Faruque, Xinzhou Yang, Shaikh Bokhtear Uddin
ETHNOPHARMACOLOGICAL RELEVANCE: Holigarna caustica (Dennst.) is commonly used in the traditional medicine to treat a variety of painful conditions such as eye irritation, inflammation, arthritis, skin diseases, cuts, and wounds. AIM OF THE STUDY: The present study was undertaken to investigate the anti-nociceptive and anti-inflammatory activities of the methanol extract of H. caustica leaves with its possible mechanism of action. MATERIALS AND METHODS: Fresh leaves of H...
January 28, 2019: Journal of Ethnopharmacology
https://read.qxmd.com/read/30703493/evaluation-of-polyherbal-ayurvedic-formulation-peedantak-vati-for-anti-inflammatory-and-analgesic-properties
#19
Acharya Balkrishna, Ravikant Ranjan, Sachin S Sakat, Vinay K Sharma, Ravikant Shukla, Khemraj Joshi, Raviraj Devkar, Niti Sharma, Sonia Saklani, Prateek Pathak, Pratima Kumari, Veena R Agarwal
ETHNOPHARMACOLOGICAL RELEVANCE: Peedantak Vati (PV) is a polyherbal ayurvedic formulation, which is regularly prescribed by the ayurvedic practitioner for the inflammatory disorders and joints pain in India. It is composed of 23 different herbs and minerals, described in ayurvedic text for their anti-inflammatory and analgesic properties. AIM OF THE STUDY: To investigate anti-inflammatory and anti-nociceptive potential of 'Peedantak Vati' using in vitro and in vivo methods...
January 28, 2019: Journal of Ethnopharmacology
https://read.qxmd.com/read/30701460/proniosomal-gel-for-transdermal-delivery-of-lornoxicam-optimization-using-factorial-design-and-in-vivo-evaluation-in-rats
#20
Hiral Shah, Anroop B Nair, Jigar Shah, Praful Bharadia, Bandar E Al-Dhubiab
OBJECTIVE: Clinical utility of lornoxicam in oral therapy is primarily restricted by the low solubility and gastric adverse effects. This study evaluated the prospective of optimized proniosomal gel to improve the clinical efficacy of lornoxicam and compare with oral therapy. METHODS: Proniosomes were formulated by coacervation phase separation technique using span 60, lecithin and cholesterol. A four-factor three-level Box-Behnken design was used to evaluate the effect of amount of four independent variables; span 60 (X1 ), cholesterol (X2 ), lecithin (X3 ) and lornoxicam (X4 ) on response variables; vesicle size (Y1 ), entrapment efficiency (Y2 ) and transdermal flux (Y3 )...
January 30, 2019: Daru: Journal of Faculty of Pharmacy, Tehran University of Medical Sciences
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