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Phosphodiesterase 4

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https://www.readbyqxmd.com/read/29331766/roflumilast-type-4-phosphodiesterase-inhibitor-attenuates-inflammation-in-rats-with-ulcerative-colitis-via-down-regulation-of-inos-and-elevation-of-camp
#1
Nahla E El-Ashmawy, Naglaa F Khedr, Hoda A El-Bahrawy, Samar A El-Adawy
BACKGROUND: Roflumilast (Rof), a phosphodiesterase 4 (PDE4) inhibitor, has been shown to be an effective agent in inflammatory diseases and marketed for chronic obstructive pulmonary disease. OBJECTIVE: This study was conducted to examine the potential anti-inflammatory effects of Rof in dextran sulphate sodium (DSS)-induced ulcerative colitis (UC) in rats and to investigate the molecular mechanisms underlying these effects. METHODS: Forty male Wistar rats were divided into four groups: normal control, colitis group (rats received 5% DSS in their drinking water continuously for 7 days), Rof group, and sulfasalazine (SLZ) group...
January 10, 2018: International Immunopharmacology
https://www.readbyqxmd.com/read/29329614/bioassay-guided-isolation-of-novel-and-selective-urease-inhibitors-from-diospyros-lotus
#2
Abdur Rauf, Ghias Uddin, Bina S Siddiqui, Ajmal Khan, Umar Farooq, Farhan A Khan, Syed Majid Bukhari, Sher Bahadar Khan
Two new dimeric naphthoquinones, 5',8'-dihydroxy-6,6'-dimethyl-7,3'-binaphthyl-1,4,1',4'-tetraone (1; Di-naphthodiospyrol D) and 5',8'-dihydroxy-5,8-dimethoxy-6,6'-dimethyl-7,3'-binaphthyl-1,4,1',4'-tetraone (2; Di-naphthodiospyrol E), along with known naphthoquinones diospyrin (3) and 8-hydroxy diospyrin (4) were isolated from the chloroform fraction of extract of Diospyros lotus roots. Their structures were elucidated by advanced spectroscopic analyses, including HSQC, HMBC, NOESY, and J-resolved NMR experiments...
November 2017: Chinese Journal of Natural Medicines
https://www.readbyqxmd.com/read/29325746/first-report-of-the-characterization-of-a-snake-venom-apyrase-ruviapyrase-from-indian-russell-s-viper-daboia-russelii-venom
#3
Bhargab Kalita, Aparup Patra, Shagufta Jahan, Ashis K Mukherjee
A novel apyrase from Russell's viper venom (RVV) was purified and characterized, and it was named Ruviapyrase (Russell's viper apyrase). It is a high molecular weight (79.4 kDa) monomeric glycoprotein that contains 2.4% neutral sugars and 58.4% N-linked oligosaccharides and strongly binds to Concanavalin A. The LC-MS/MS analysis did not identify any protein in NCBI protein database, nevertheless some de novo sequences of Ruviapyrase showed putative conserved domain of apyrase superfamily. Ruviapyrase hydrolysed adenosine triphosphate (ATP) to a significantly greater extent (p < ...
January 8, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29325221/naphthalene-derivatives-and-quinones-from-ventilago-denticulata-and-their-nitric-oxide-radical-scavenging-antioxidant-cytotoxic-antibacterial-and-phosphodiesterase-inhibitory-activities
#4
Wannapha Molee, Anuchit Phanumartwiwath, Chatchai Kesornpun, Sanya Sureram, Nattaya Ngamrojanavanich, Kornkanok Ingkaninan, Chulabhorn Mahidol, Somsak Ruchirawat, Prasat Kittakoop
New naphthalene derivatives (1 and 2) and a new isomer (3) of ventilagolin, together with known anthraquinones, chrysophanol (4), physcion or emodin 3-methyl ether (5), and emodin (6), were isolated from vines of Ventilago denticulata. The isolated compounds exhibited cytotoxic activity with IC50 values of 1.15-40.54 μg/mL. Compounds 1-3 selectively exhibited weak antibacterial activity (MIC values of 200.0-400.0 μg/mL), while emodin (6) displayed moderate antibacterial activity with MIC values of 25.0 μg/mL...
January 11, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29301136/assessment-of-the-airway-smooth-muscle-relaxant-effect-of-drotaverine
#5
Zoltán Patai, András Guttman, Endre G Mikus
BACKGROUND: Drotaverine, a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor, blocks the degradation of 3',5'-cyclic adenosine monophosphate. However, published receptor binding data showed that drotaverin also binds to the L-type voltage-operated calcium channel (L-VOCC). Based on these molecular mechanisms of action, a direct and indirect (by blocking the constrictor response) relaxant effect on airway smooth muscle can be predicted, which has not yet been assessed. SUMMARY: Accordingly, drotaverine and reference agents were tested both on the histamine-, methacholine-, or KCl-induced contraction response and on precontracted guinea pig tracheal preparations...
January 4, 2018: Pharmacology
https://www.readbyqxmd.com/read/29298510/structural-activity-relationship-of-ginsenosides-from-steamed-ginseng-in-the-treatment-of-erectile-dysfunction
#6
Ang Ying, Qing-Tao Yu, Li Guo, Wen-Song Zhang, Jin-Feng Liu, Yun Li, Hong Song, Ping Li, Lian-Wen Qi, Ya-Zhong Ge, E-Hu Liu, Qun Liu
Ginseng has been reported to have diverse pharmacological effects. One of the therapeutic claims for ginseng is to enhance sexual function. Ginsenosides are considered as the major active constituents. A steaming process can alter the ginsenoside profile of ginseng products. The structure-function relationship of ginsenosides in the treatment of erectile dysfunction (ED) has not been investigated yet. In this work, 15 different processed ginsengs are produced by steaming, and 13 major ginsensosides are quantified by liquid chromatography with UV detection, including Rg1, Re, Rf, Rb1, Rc, Rb2, Rf, Rk3, Rh4, 20S-Rg3, 20R-Rg3, Rk1, and Rg5...
January 3, 2018: American Journal of Chinese Medicine
https://www.readbyqxmd.com/read/29291443/prenylated-flavonoids-as-potent-phosphodiesterase-4-inhibitors-from-morus-alba-isolation-modification-and-structure-activity-relationship-study
#7
Yan-Qiong Guo, Gui-Hua Tang, Lan-Lan Lou, Wei Li, Bei Zhang, Bo Liu, Sheng Yin
The bioassay-guided phytochemical study of a traditional Chinese medicine Morus alba led to the isolation of 18 prenylated flavonoids (1-18), of which (±)-cyclomorusin (1/2), a pair of enantiomers, and 14-methoxy-dihydromorusin (3) are the new ones. Subsequent structural modification of the selected components by methylation, esterification, hydrogenation, and oxidative cyclization led to 14 more derivatives (19-32). The small library was screened for its inhibition against phosphodiesterase-4 (PDE4), which is a drug target for the treatment of asthma and chronic obstructive pulmonary disease (COPD)...
December 16, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29290010/computer-aided-design-of-multi-target-ligands-at-a1r-a2ar-and-pde10a-key-proteins-in-neurodegenerative-diseases
#8
Leen Kalash, Cristina Val, Jhonny Azuaje, María I Loza, Fredrik Svensson, Azedine Zoufir, Lewis Mervin, Graham Ladds, José Brea, Robert Glen, Eddy Sotelo, Andreas Bender
Compounds designed to display polypharmacology may have utility in treating complex diseases, where activity at multiple targets is required to produce a clinical effect. In particular, suitable compounds may be useful in treating neurodegenerative diseases by promoting neuronal survival in a synergistic manner via their multi-target activity at the adenosine A1 and A2A receptors (A1R and A2AR) and phosphodiesterase 10A (PDE10A), which modulate intracellular cAMP levels. Hence, in this work we describe a computational method for the design of synthetically feasible ligands that bind to A1 and A2A receptors and inhibit phosphodiesterase 10A (PDE10A), involving a retrosynthetic approach employing in silico target prediction and docking, which may be generally applicable to multi-target compound design at several target classes...
December 30, 2017: Journal of Cheminformatics
https://www.readbyqxmd.com/read/29286075/genome-expression-profiling-predicts-the-molecular-mechanism-of-peripheral-myelination
#9
Xiaoming Wu
The present study aimed to explore the molecular mechanism of myelination in the peripheral nervous system (PNS) based on genome expression profiles. Microarray data (GSE60345) was acquired from the Gene Expression Omnibus database. Differentially expressed genes (DEGs) were integrated and subsequently subjected to pathway and term enrichment analysis. A protein‑protein interaction network was constructed and the top 200 DEGs according to their degree value were further subjected to pathway enrichment analysis...
December 22, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/29277585/a-comparison-of-time-taken-to-return-to-baseline-erectile-function-following-focal-and-whole-gland-ablative-therapies-for-localized-prostate-cancer-a-systematic-review
#10
REVIEW
Nicholas A Faure Walker, Joseph M Norris, Taimur T Shah, Tet Yap, Paul Cathcart, Caroline M Moore, Hashim U Ahmed, Mark Emberton, Suks Minhas
OBJECTIVES: To systematically review erectile function (EF) outcomes following primary whole gland (WG) and focal ablative therapies for localized prostate cancer to ascertain whether the treatment modality or intended treatment volume affects the time taken to recover baseline EF. METHOD AND MATERIALS: A systematic review was performed according to the preferred reporting items for systematic review and meta-analysis statement. Inclusion criteria were men with localized prostate cancer treated with primary, ablative therapy...
December 22, 2017: Urologic Oncology
https://www.readbyqxmd.com/read/29277372/effects-of-chlorogenic-acid-on-carbachol-induced-contraction-of-mouse-urinary-bladder
#11
Takeharu Kaneda, Noriyasu Sasaki, Norimoto Urakawa, Kazumasa Shimizu
Chlorogenic acid (CGA) is a polyphenol found in coffee and medicinal herbs such as Lonicera japonica. In this study, the effect of CGA-induced relaxation on carbachol (CCh)-induced contraction of mouse urinary bladder was investigated. CGA (30-300 μg/ml) inhibited CCh- or U46619-induced contraction in a concentration-dependent manner. SQ22536 (adenylyl cyclase inhibitor) recovered CGA-induced relaxation of CCh-induced contraction; however, ODQ (guanylyl cyclase inhibitor) did not have the same effect. In addition, 3-isobutyl-1-methylxanthine (IBMX) enhanced CGA-induced relaxation; however, forskolin or sodium nitroprusside did not have the same effect...
December 15, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29275958/edeus-a-real-life-study-on-the-users-of-phosphodiesterase-type-5-inhibitors-prevalence-perceptions-and-health-care-seeking-behavior-among-european-men-with-a-focus-on-2nd-generation-avanafil
#12
Giovanni Corona, Mario Maggi, Emmanuele A Jannini
INTRODUCTION: Erectile dysfunction (ED) is a multidimensional disorder with an estimated prevalence of 1% to 10% in men younger than 40 years and up to 100% in men in their 70s and 80s. AIM: To evaluate the real-life characteristics and unmet needs of men with ED, its impact on well-being, and treatment rates across Europe. METHODS: Adult men in Belgium, France, Germany, Italy, Poland, Portugal, and Spain were invited to participate in the survey...
December 21, 2017: Sexual Medicine
https://www.readbyqxmd.com/read/29273417/an-appraisal-on-synthetic-and-pharmaceutical-perspectives-of-pyrazolo-4-3-d-pyrimidine-scaffold
#13
REVIEW
Srinivasulu Cherukupalli, Girish A Hampannavar, Sampath Chinnam, Balakumar Chandrasekaran, Nisar Sayyad, Francis Kayamba, Rajeshwar Reddy Aleti, Rajshekhar Karpoormath
Pyrazolo[4,3-d]pyrimidine, a fused heterocycle bearing pyrazole and pyrimidine portions has gained a significant attention in the field of bioorganic and medicinal chemistry. Pyrazolo[4,3-d]pyrimidine derivatives have demonstrated numerous pharmacological activities particularly, anti-cancer, anti-infectious, phosphodiesterase inhibitors, adenosine antagonists and cytokinin antagonists etc. This review extensively unveils the synthetic and pharmacological diversity with special emphasis on structural variations around pyrazolo[4,3-d]pyrimidine scaffold...
October 25, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29260411/malignancy-risk-and-recurrence-with-psoriasis-and-its-treatments-a-concise-update
#14
REVIEW
Shamir Geller, Haoming Xu, Mark Lebwohl, Beatrice Nardone, Mario E Lacouture, Meenal Kheterpal
Psoriasis is a common inflammatory cutaneous disease that affects approximately 120 million people worldwide. Systemic treatments have significantly improved disease burden, but concerns persist regarding their association with increased risk of malignancy. Patients with psoriasis have a slightly elevated baseline risk of lymphoproliferative diseases. Studies on methotrexate and cyclosporine, as well as older biological agents such as tumor necrosis factor inhibitors, have found no increased risk of non-cutaneous solid tumors; however, positive associations between cutaneous squamous cell carcinomas and certain therapies have been found...
December 19, 2017: American Journal of Clinical Dermatology
https://www.readbyqxmd.com/read/29248522/phosphodiesterase-4-pde4-inhibitors
#15
Rema Zebda, Amy S Paller
Historically, drugs available for treating atopic dermatitis (AD) have been limited to topical corticosteroids (TCS) and topical calcineurin inhibitors (TCI), with systemic immunosuppressants and phototherapy reserved for severe AD. Despite their efficacy, with long term use, these agents have associated safety concerns and limitations. More targeted options with fewer systemic and cutaneous side effects are needed for treating atopic dermatitis. Phosphodiesterase 4 is involved in the regulation of proinflammatory cytokines via the degradation of cAMP...
December 14, 2017: Journal of the American Academy of Dermatology
https://www.readbyqxmd.com/read/29246942/synergistic-targeting-of-the-regulatory-and-catalytic-subunits-of-pi3k%C3%AE-in-mature-b-cell-malignancies
#16
Jeffrey Cooney, An-Ping Lin, Daifeng Jiang, Long Wang, Avvaru N Suhasini, Jamie Myers, ZhiJun Qiu, Albert Wölfler, Heinz Sill, Ricardo C T Aguiar
PURPOSE: Aberrant activation of the B cell receptor (BCR) is implicated in the pathogenesis of mature B-cell tumors, a concept validated in part by the clinical success of inhibitors of the BCR-related kinases BTK (Bruton's tyrosine kinase) and PI3Kδ (Phosphatidylinositol-4,5-bisphosphate 3-kinase delta). These inhibitors have limitations, including the paucity of complete responses, acquired resistance, and toxicity. Here we examined the mechanism by which the cyclic-AMP/PDE4 signaling axis suppresses PI3K, towards identifying a novel mechanism-based combinatorial strategy to attack BCR-dependency in mature B-cell malignancies...
December 15, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/29244957/hypercementosis-associated-with-enpp1-mutations-and-gaci
#17
V Thumbigere-Math, A Alqadi, N I Chalmers, M B Chavez, E Y Chu, M T Collins, C R Ferreira, K FitzGerald, R I Gafni, W A Gahl, K S Hsu, M S Ramnitz, M J Somerman, S G Ziegler, B L Foster
Mineralization of bones and teeth is tightly regulated by levels of extracellular inorganic phosphate (Pi) and pyrophosphate (PPi). Three regulators that control pericellular concentrations of Pi and PPi include tissue-nonspecific alkaline phosphatase (TNAP), progressive ankylosis protein (ANK), and ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1). Inactivation of these factors results in mineralization disorders affecting teeth and their supporting structures. This study for the first time analyzed the effect of decreased PPi on dental development in individuals with generalized arterial calcification of infancy (GACI) due to loss-of-function mutations in the ENPP1 gene...
December 1, 2017: Journal of Dental Research
https://www.readbyqxmd.com/read/29242380/insights-into-the-proteome-of-gastrointestinal-stromal-tumors-derived-exosomes-reveals-new-potential-diagnostic-biomarkers
#18
Safinur Atay, Daniel W Wilkey, Mohammed M Milhem, Michael Merchant, Andrew K Godwin
Developing tumors continuously release nano-sized vesicles that represent circulating "fingerprints" of the tumor's identity.  In gastrointestinal stromal tumor (GIST), we have previously reported that these tumors release "oncosomes" carrying the constitutively activated tyrosine kinase (TK) receptor KIT.  Despite the clinical utility of TK inhibitors, such as imatinib mesylate (IM), recurrence and metastasis are clinical problems that urge the need to identify new tumor-derived molecules.  To this aim, we performed the first high quality proteomic study of GIST-derived exosomes (GDEs) and identified 1,060 proteins composing the core GDE proteome (cGDEp)...
December 14, 2017: Molecular & Cellular Proteomics: MCP
https://www.readbyqxmd.com/read/29241652/acute-administration-of-roflumilast-enhances-immediate-recall-of-verbal-word-memory-in-healthy-young-adults
#19
M A Van Duinen, A Sambeth, P R A Heckman, S Smit, M Tsai, G Lahu, T Uz, A Blokland, J Prickaerts
The need for new and effective treatments for dementia remains indisputably high. Phosphodiesterase inhibitors (PDE-Is) have proven efficacy as cognitive enhancers based on their positive effects in numerous preclinical studies. Especially the PDE4 subfamily is of interest due to its expression in the hippocampus, the key structure for memory formation. The current study investigates the memory enhancing effects of the clinically approved PDE4-I roflumilast in a test battery including the Verbal Learning Task (VLT) combined with electroencephalography (EEG) recording...
December 11, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29233027/effects-of-phosphodiestrase-type-5-inhibitors-in-epinephrine-induced-arrhythmia-in-rats-involvement-of-lactate-dehydrogenase-and-creatine-kinase-downregulation-and-adiponectin-expression
#20
Aaa Salama, R E Mostafa, E A Omara
Cardiac arrhythmia is a common cause of mortality, and its progression may be due to abnormal sympathetic nerve activity and catecholamine release. Besides, lactate dehydrogenase (LDH) and creatine kinase (CK) downregulation and adiponectin expression play important roles in promoting coronary artery disease. The study aimed to examine the possible cardioprotective effect of members of phosphodiesterase type 5 (PDE-5) inhibitors in epinephrine-induced arrhythmia in rats. Arrhythmia was induced by cumulative boluses of epinephrine (4, 8, 16, 32, 64, and 128 mg/kg) given at 10-min intervals...
January 1, 2017: Human & Experimental Toxicology
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