keyword
MENU ▼
Read by QxMD icon Read
search

PDE inhibitor.

keyword
https://www.readbyqxmd.com/read/28443667/identification-of-a-phosphodiesterase-inhibiting-fraction-from-roasted-coffee-coffea-arabica-through-activity-guided-fractionation
#1
Teresa Röhrig, David Liesenfeld, Elke Richling
Recent reports that coffee can significantly inhibit cAMP phosphodiesterases (PDE) in vitro, as well as in vivo, have added another beneficial effect of coffee consumption. However, the PDE-inhibiting substances remain mostly unknown. We chose activity-guided fractionation and an in vitro test system to identify the coffee components responsible for PDE inhibition. This approach indicated that a fraction of melanoidins reveals strong PDE inhibiting potential (IC50 = 130 ± 42 µg/mL). These melanoidins were characterized as water soluble, low molecular weight melanoidins (< 3kDa) with a nitrogen content of 4...
April 26, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28424739/rapid-screening-of-potential-phosphodiesterase-inhibitors-from-the-roots-of-ilex-pubescens-hook-et-arn-using-a-combination-of-ultrafiltration-and-lc-ms
#2
Zichen Liu, Zongtao Lin, Shizhong Chen, Lingjun Wang, Shaoxiang Xian
The cyclic nucleotide phosphodiesterase (PDE) plays an important role in regulating the levels of second messenger molecules cAMP and cGMP. Various PDE inhibitors have been successfully developed into drugs for targeted diseases. In addition, PDE inhibitors can also be found in different foods and natural medicines. In this study, ultrafiltration liquid chromatography-diode-array detector-electrospray ionization-ion-trap-time-of-flight-mass spectrometry (ultrafiltration LC-DAD-ESI-IT-TOF-MS) was applied to screen PDE inhibitors from the roots of Ilex pubescens Hook...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/28421158/cytotoxicity-of-zardaverine-in-embryonal-rhabdomyosarcoma-from-a-costello-syndrome-patient
#3
Donna M Cartledge, Katherine M Robbins, Katherine M Drake, Rachel Sternberg, Deborah L Stabley, Karen W Gripp, E Anders Kolb, Katia Sol-Church, Andrew D Napper
Costello syndrome (CS) patients suffer from a very high 10% incidence of embryonal rhabdomyosarcoma (ERMS). As tools to discover targeted therapeutic leads, we used a CS patient-derived ERMS cell line (CS242 ERMS) harboring a homozygous p.G12A mutation in HRAS, and a control cell line derived from the same patient comprising non-malignant CS242 fibroblasts with a heterozygous p.G12A HRAS mutation. A library of 2,000 compounds with known pharmacological activities was screened for their effect on CS242 ERMS cell viability...
2017: Frontiers in Oncology
https://www.readbyqxmd.com/read/28414142/doxofylline-does-not-increase-formoterol-induced-camp-nor-mkp-1-expression-in-asm-cells-resulting-in-lack-of-anti-inflammatory-effect
#4
Brijeshkumar S Patel, Michael J Kugel, Gina Baehring, Alaina J Ammit
The xanthine doxofylline has been examined in clinical trials and shown to have efficacy and greater tolerability than theophylline in asthma and chronic obstructive pulmonary disease. The 'novofylline' doxofylline has demonstrated bronchodilatory and anti-inflammatory actions in in vivo and ex vivo experimental models of respiratory disease. However, there are limited studies in vitro. We address this herein and examine whether doxofylline has anti-inflammatory impact on primary cultures of airway smooth muscle (ASM) cells...
April 13, 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28406621/discovery-of-selective-phosphodiesterase-1-inhibitors-with-memory-enhancing-properties
#5
Brian Dyck, Bryan Branstetter, Tawfik Gharbaoui, Andrew R Hudson, J Guy Breitenbucher, Laurent Gomez, Iriny Botrous, Tami Marrone, Richard Barido, Charles K Allerston, E Peder Cedervall, Rui Xu, Vandana Sridhar, Ryan Barker, Kathleen Aertgeerts, Kara Schmelzer, David Neul, Dong Lee, Mark Eben Massari, Carsten B Andersen, Kristen Sebring, Xianbo Zhou, Robert Petroski, James Limberis, Martin Augustin, Lawrence E Chun, Thomas E Edwards, Marco Peters, Ali Tabatabaei
A series of potent thienotriazolopyrimidinone-based PDE1 inhibitors was discovered. X-ray crystal structures of example compounds from this series in complex with the catalytic domain of PDE1B and PDE10A were determined, allowing optimization of PDE1B potency and PDE selectivity. Reduction of hERG affinity led to greater than a 3000-fold selectivity for PDE1B over hERG. 6-(4-Methoxybenzyl)-9-((tetrahydro-2H-pyran-4-yl)methyl)-8,9,10,11-tetrahydropyrido[4',3':4,5]thieno[3,2-e][1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-one was identified as an orally bioavailable and brain penetrating PDE1B enzyme inhibitor with potent memory-enhancing effects in a rat model of object recognition memory...
April 13, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28394532/-phosphodiesterase-type-5-inhibitors-in-the-treatment-of-erectile-dysfunction-past-present-and-future
#6
S I Gamidov, R I Ovchinnikov, A Yu Popova, S Kh Izhbaev
This review article describes the differences in efficacy and side effects between available phosphodiesterase type 5 (PDE-5) inhibitors used for treating erectile dysfunction. The most studied PDE-5 inhibitor is sildenafil.
April 2017: Urologii︠a︡
https://www.readbyqxmd.com/read/28382232/resveratrol-enhances-the-inotropic-effect-but-inhibits-the-proarrhythmic-effect-of-sympathomimetic-agents-in-rat-myocardium
#7
Jesús Hernandez-Cascales
BACKGROUND: Resveratrol is a cardioprotective agent with known antiarrhythmic effects that has recently been shown to inhibit phosphodiesterase (PDE) enzyme activity. Thus, it is possible that resveratrol increases the inotropic effect of sympathomimetic agents, as PDE inhibitors do but, unlike other PDE inhibitors, its effect may not be accompanied by proarrhythmia due to its antiarrhythmic action. This work is aimed to test this hypothesis. METHODS: This is an "in vitro" concentration-response relationship study...
2017: PeerJ
https://www.readbyqxmd.com/read/28379598/sildenafil-associated-hepatoxicity-a-review-of-the-literature
#8
S Graziano, A Montana, S Zaami, M C Rotolo, A Minutillo, F P Busardò, E Marinelli
Sildenafil citrate (Viagra®) is a vasoactive agent available worldwide since 1998 for the treatment of male erectile dysfunction. It is a selective phosphodiesterase type 5-enzyme inhibitor able to potentiate the downstream effects of nitric oxide on smooth muscle relaxation and vasodilation through its effects on the cyclic guanosine monophosphate (c-GMP) pathway in the erectile tissue of the penis. When sildenafil is orally administered, it is rapidly absorbed with a maximum plasma concentration achieved within 1 h and has a terminal half-life of between 3 to 6 h...
March 2017: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/28359014/sperm-motility-activation-in-the-critically-endangered-booroolong-frog-the-effect-of-medium-osmolality-and-phosphodiesterase-inhibitors
#9
Aimee J Silla, Leesa M Keogh, Phillip G Byrne
Effective activation of sperm motility is fundamental to successful artificial fertilisation; however, studies investigating optimal procedures in amphibians are lacking. This study found the optimal osmolality of activation media for sperm motility activation and evaluated the effect of phosphodiesterase (PDE) inhibitors on sperm activation and longevity in the critically endangered booroolong frog, Litoria booroolongensis. To assess the effect of medium osmolality (10, 25, 50, 75, 100 and 200mOsmolkg-1) and PDE inhibitors (control, 2...
March 31, 2017: Reproduction, Fertility, and Development
https://www.readbyqxmd.com/read/28349188/-erectile-dysfunction-current-diagnostics-and-treatment
#10
C Leiber
Erectile dysfunction is a medical disease with extensive influence on the quality of life and well-being of patients and their female or male partners. Nowadays, most of the underlying pathological factors are well known. The general medical history with the question of possible risk factors and the specific sexual history play the most important roles in the guideline-based diagnostics. In addition, a thorough clinical examination and specific laboratory tests should be carried out. Phosphodiesterase 5 (PDE-5) inhibitors, vacuum devices, injection therapy and penile prostheses are the options for an evidence-based and individual treatment of affected patients...
April 2017: Der Urologe. Ausg. A
https://www.readbyqxmd.com/read/28348070/syndecan-1-represses-cell-growth-and-fsh-responsiveness-in-human-granulosa-cells
#11
Simon Colombe, Laura Houllier, Emmanuelle Fleurot, Guénaëlle Levallet, Annie BenhaÏm, Pierre-Jacques Bonnamy, Jerome Levallet
Albeit devoid of intrinsic catalytic activity, the transmembrane heparan sulfate proteoglycan syndecan 1 plays critical roles in cellular processes such as extracellular matrix crosstalk, cytoskeletal organization, cell spreading, proliferation and differentiation. During the ovarian cycle, the expression of syndecan 1 in granulosa cells shows cyclic variation suggesting that it might fulfil specific roles in follicle development. To investigate its physiological roles on granulosa cells, syndecan 1 was overexpressed in human granulosa cell line KGN which retains features of granulosa cells from small antral follicle such as estradiol (E2) synthesis and low expression of functional FSH receptor (FSHR)...
March 27, 2017: Reproduction: the Official Journal of the Society for the Study of Fertility
https://www.readbyqxmd.com/read/28338622/phosphodiesterase-inhibitors-as-a-therapeutic-approach-to-neuroprotection-and-repair
#12
REVIEW
Eric P Knott, Mazen Assi, Sudheendra N R Rao, Mousumi Ghosh, Damien D Pearse
A wide diversity of perturbations of the central nervous system (CNS) result in structural damage to the neuroarchitecture and cellular defects, which in turn are accompanied by neurological dysfunction and abortive endogenous neurorepair. Altering intracellular signaling pathways involved in inflammation and immune regulation, neural cell death, axon plasticity and remyelination has shown therapeutic benefit in experimental models of neurological disease and trauma. The second messengers, cyclic adenosine monophosphate (cyclic AMP) and cyclic guanosine monophosphate (cyclic GMP), are two such intracellular signaling targets, the elevation of which has produced beneficial cellular effects within a range of CNS pathologies...
March 24, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28337525/phosphodiesterase-1b-pde1b-knockout-mice-are-resistant-to-forced-swim-and-tail-suspension-induced-immobility-and-show-upregulation-of-pde10a
#13
Jillian R Hufgard, Michael T Williams, Matthew R Skelton, Olivera Grubisha, Filipa M Ferreira, Helen Sanger, Mary E Wright, Tracy M Reed-Kessler, Kurt Rasmussen, Ronald S Duman, Charles V Vorhees
RATIONALE: Major depressive disorder is a leading cause of suicide and disability. Despite this, current antidepressants provide insufficient efficacy in more than 60% of patients. Most current antidepressants are presynaptic reuptake inhibitors; postsynaptic signal regulation has not received as much attention as potential treatment targets. OBJECTIVES: We examined the effects of disruption of the postsynaptic cyclic nucleotide hydrolyzing enzyme, phosphodiesterase (PDE) 1b, on depressive-like behavior and the effects on PDE1B protein in wild-type (WT) mice following stress...
March 23, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28330503/caffeine-modulates-glucocorticoid-induced-expression-of-ctgf-in-lung-epithelial-cells-and-fibroblasts
#14
Markus Fehrholz, Kirsten Glaser, Christian P Speer, Silvia Seidenspinner, Barbara Ottensmeier, Steffen Kunzmann
BACKGROUND: Although caffeine and glucocorticoids are frequently used to treat chronic lung disease in preterm neonates, potential interactions are largely unknown. While anti-inflammatory effects of glucocorticoids are well defined, their impact on airway remodeling is less characterized. Caffeine has been ascribed to positive effects on airway inflammation as well as remodeling. Connective tissue growth factor (CTGF, CCN2) plays a key role in airway remodeling and has been implicated in the pathogenesis of chronic lung diseases such as bronchopulmonary dysplasia (BPD) in preterm infants...
March 23, 2017: Respiratory Research
https://www.readbyqxmd.com/read/28316997/sildenafil-can-affect-innate-and-adaptive-immune-system-in-both-experimental-animals-and-patients
#15
REVIEW
Monika Kniotek, Agnieszka Boguska
Sildenafil, a type 5 phosphodiesterase inhibitor (PDE5-I), is primarily used for treating erectile dysfunction. Sildenafil inhibits the degradation of cyclic guanosine monophosphate (cGMP) by competing with cGMP for binding site of PDE5. cGMP is a secondary messenger activating protein kinases and a common regulator of ion channel conductance, glycogenolysis, and cellular apoptosis. PDE5 inhibitors (PDE-Is) found application in cardiology, nephrology, urology, dermatology, oncology, and gynecology. Positive result of sildenafil treatment is closely connected with its immunomodulatory effects...
2017: Journal of Immunology Research
https://www.readbyqxmd.com/read/28306529/in-vitro-inhibition-of-phosphodiesterase-5-and-arginase-activities-from-rat-penile-tissue-by-two-nigerian-herbs-hunteria-umbellata-and-anogeissus-leiocarpus
#16
Ganiyu Oboh, Adeniyi Abiodun Adebayo, Ayokunle Olubode Ademosun, Aline August Boligon
BACKGROUND: Anogeissus leiocarpus and Hunteria umbellata have been reportedly used in traditional medicine for the management of erectile dysfunction (ED). However, the scientific basis for their use has not been well established. Therefore, this study was designed to investigate the inhibitory effects of water extractable phytochemicals of H. umbellata and A. leiocarpus on phosphodiesterase-5 (PDE-5) and arginase as well as pro-oxidants induced lipid peroxidation in rat penile tissue...
March 17, 2017: Journal of Basic and Clinical Physiology and Pharmacology
https://www.readbyqxmd.com/read/28302034/co-morbid-erectile-dysfunction-ed-and-antidepressant-treatment-in-a-patient-a-management-challenge
#17
Maszaidi Zainol, Hatta Sidi, Jaya Kumar, Srijit Das, Shaiful Ismail, Muhammad Hizri Hatta, Najwa Baharudin, Arun Ravindran
Across the globe, antidepressants (AD) and phosphodiesterase-5 inhibitors (PDE-5i) are commonly prescribed psychopharmacological agents for patients with co-morbid mental-health problem and sexual dysfunction (SD). The serotonergic and/or noradrenergic ADs, although is an effective agent are not without SD side-effects, especially erectile dysfunction (ED). ED is an inability to achieve, or maintain an erection for satisfactory sexual intercourse during the phases of male's sexual arousal. It is recognized as an important reason why non-adherence to treatment was observed in patients who are on AD...
March 15, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28267871/effect-of-bucladesine-pentoxifylline-and-h-89-as-cyclic-adenosine-monophosphate-analog-phosphodiesterase-and-protein-kinase-a-inhibitor-on-acute-pain
#18
Forouz Salehi, Mahshid Sadat Hosseini-Zare, Haleh Aghajani, Yalda Seyedi, Maryam Sadat Hosseini-Zare, Mohammad Sharifzadeh
The aim of the present study was to determine the effects of Cyclic adenosine monophosphate (cAMP) and its dependent pathway on thermal nociception in a mouse model of acute pain. Here we studied the effect of H-89 (protein kinase A inhibitor), Bucladesine (Db-cAMP) (membrane permeable analog of cAMP) and pentoxifylline (PTX) (non-specific phosphodiesterase (PDE) inhibitor) on pain sensation. Different doses of H-89 (0.05, 0.1 and 0.5 mg/100g), PTX (5, 10 and 20 mg/100g), and Db-cAMP (50, 100 and 300 nM/mouse) were administered intraperitoneally (I...
March 7, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28263828/6-hydroxy-5-7-dimethoxy-flavone-suppresses-the-neutrophil-respiratory-burst-via-selective-pde4-inhibition-to-ameliorate-acute-lung-injury
#19
Yung-Fong Tsai, Tzu-Chi Chu, Wen-Yi Chang, Yang-Chang Wu, Fang-Rong Chang, Shun-Chin Yang, Tung-Ying Wu, Yu-Ming Hsu, Chun-Yu Chen, Shih-Hsin Chang, Tsong-Long Hwang
Over-activated neutrophils produce enormous oxidative stress and play a key role in the development of acute and chronic inflammatory diseases. 6-Hydroxy-5,7-dimethoxy-flavone (UFM24), a flavone isolated from the Annonaceae Uvaria flexuosa, showed inhibitory effects on human neutrophil activation and salutary effects on lipopolysaccharide (LPS)-induced acute lung injury (ALI) in mice. UFM24 potently inhibited superoxide anion (O2(•-)) generation, reactive oxidants, and CD11b expression, but not elastase release, in N-formyl-l-methionyl-l-leucyl-l-phenylalanine (fMLF)-activated human neutrophils...
March 3, 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28258674/ibudilast-a-non%C3%A2-selective-phosphodiesterase-inhibitor-in-brain-disorders
#20
Joanna Schwenkgrub, Małgorzata Zaremba, Dagmara Mirowska-Guzel, Iwona Kurkowska-Jastrzębska
Ibudilast (IBD) is a non‑selective (3, 4, 10, 11) phosphodiesterase (PDE) inhibitor, used mainly as a bronchodilator for the treatment of bronchial asthma. PDE play a central role in cellular function (e.g. differentiation, synaptic plasticity and inflammatory response) by metabolizing cyclic nucleotides. The results from preclinical and clinical studies indicate that IBD has a broader range of action through suppression of pro‑inflammatory cytokines (IL‑6, IL‑1β, TNF‑α), toll‑like receptor 4 blockade (TLR‑4), inhibition of a macrophage migration inhibitory factor (MIF), up‑regulation the anti‑inflammatory cytokine (IL‑10), and promotion of neurotrophic factors (GDNF, NGF, NT‑4)...
March 2, 2017: Postȩpy Higieny i Medycyny Doświadczalnej
keyword
keyword
36620
1
2
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"