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https://www.readbyqxmd.com/read/28709568/current-and-emerging-topical-therapies-for-atopic-dermatitis
#1
Jeremy Udkoff, Andrea Waldman, Jusleen Ahluwalia, Jenna Borok, Lawrence F Eichenfield
The pathogenesis of atopic dermatitis (AD) involves epidermal barrier dysfunction and T helper cell type 2 (Th2) lymphocyte-driven inflammation. Cytokines, such as interleukin 4 (IL-4) and IL-13, are important in this reaction. They stimulate B cells to produce immunoglobulin E, causing atopic disease. This process has been well characterized, and new therapies for AD, such as phosphodiesterase 4 (PDE-4) inhibitors, Th2-expressed chemoattractant receptor-homologous molecule antagonists, and Janus kinase inhibitors, work by antagonizing this cellular pathway...
July 2017: Clinics in Dermatology
https://www.readbyqxmd.com/read/28706457/relaxant-and-anti-inflammatory-effect-of-two-thalidomide-analogs-as-pde-4-inhibitors-in-pregnant-rat-uterus
#2
Víctor Manuel Muñoz-Pérez, Eduardo Fernández-Martínez, Héctor Ponce-Monter, Mario I Ortiz
The aim of this study was to evaluate the relaxant and anti-inflammatory effects of two thalidomide analogs as phosphodiesterase-4 (PDE-4) inhibitors in pregnant rat uterus. Uteri from Wistar female rats were isolated at 19 day of pregnancy. Uterine samples were used in functional studies to evaluate the inhibitory effects of the thalidomide analogs, methyl 3-(4-nitrophthalimido)-3-(3,4-dimethoxyphenyl)-propanoate (4NO2PDPMe) and methyl 3-(4-aminophthalimido)-3-(3,4-dimethoxyphenyl)-propanoate (4APDPMe), on prostaglandin-F2α (PGF2α)-induced phasic, K(+)-induced tonic, and Ca(2+)-induced contractions...
July 2017: Korean Journal of Physiology & Pharmacology
https://www.readbyqxmd.com/read/28704396/phenotypic-chemical-and-functional-characterization-of-cyclic-nucleotide-phosphodiesterase-4-pde4-as-a-potential-anthelmintic-drug-target
#3
Thavy Long, Liliana Rojo-Arreola, Da Shi, Nelly El-Sakkary, Kurt Jarnagin, Fernando Rock, Maliwan Meewan, Alberto A Rascón, Lin Lin, Katherine A Cunningham, George A Lemieux, Larissa Podust, Ruben Abagyan, Kaveh Ashrafi, James H McKerrow, Conor R Caffrey
BACKGROUND: Reliance on just one drug to treat the prevalent tropical disease, schistosomiasis, spurs the search for new drugs and drug targets. Inhibitors of human cyclic nucleotide phosphodiesterases (huPDEs), including PDE4, are under development as novel drugs to treat a range of chronic indications including asthma, chronic obstructive pulmonary disease and Alzheimer's disease. One class of huPDE4 inhibitors that have yielded marketed drugs is the benzoxaboroles (Anacor Pharmaceuticals)...
July 13, 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/28701498/phosphodiesterase-4-rethinking-cognition-in-parkinson-disease
#4
EDITORIAL
Claudia Jacova, Stewart A Factor
No abstract text is available yet for this article.
July 12, 2017: Neurology
https://www.readbyqxmd.com/read/28701494/loss-of-phosphodiesterase-4-in-parkinson-disease-relevance-to-cognitive-deficits
#5
Flavia Niccolini, Heather Wilson, Gennaro Pagano, Christopher Coello, Mitul A Mehta, Graham E Searle, Roger N Gunn, Eugenii A Rabiner, Thomas Foltynie, Marios Politis
OBJECTIVE: To assess in vivo the expression of phosphodiesterase 4 (PDE4) and its relevance to cognitive symptoms in patients with Parkinson disease (PD) using [(11)C]rolipram PET. METHODS: We studied 12 levodopa-treated patients with PD with no concurrent diagnosis of mild cognitive impairment or dementia. Their data were compared with those from 12 healthy controls. All participants underwent neuropsychiatric and cognitive assessment using the Cambridge Neuropsychological Test Automated Battery...
July 12, 2017: Neurology
https://www.readbyqxmd.com/read/28700469/microarray-analysis-of-copy-number-variations-and-gene-expression-profiles-in-prostate-cancer
#6
Yuping Han, Xuefei Jin, Hongyan Li, Kaichen Wang, Ji Gao, Lide Song, Yanting Lv
BACKGROUND: This study aimed to identify potential prostate cancer (PC)-related variations in gene expression profiles. METHODS: Microarray data from the GSE21032 dataset that contained the whole-transcript and exon-level expression profile (GSE21034) and Agilent 244K array-comparative genomic hybridization data (GSE21035) were downloaded from the Gene Expression Omnibus database. Differentially expressed genes (DEGs) and copy-number variations (CNVs) were identified between PC and normal tissue samples...
July 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28698053/stable-c-n-axial-chirality-in-1-aryluracil-scaffold-and-differences-in-in-vitro-metabolic-clearance-between-atropisomers-of-pde4-inhibitor
#7
Futoshi Hasegawa, Kazushi Kawamura, Hiroshi Tsuchikawa, Michio Murata
We report herein the stable C-N axial chirality in a 1-phenyl-6-aminouracil scaffold owing to the presence of various functional groups at the ortho-position of the N(1)-phenyl group. Racemic 1-phenyl-6-aminouracils were first separated by chiral HPLC or converting them to the corresponding diastereomers using a chiral resolving agent. We then determined the rotational barrier of each atropisomer by a thermal racemization method and found that these compounds have rotational barriers similar to other C-N axially chiral biaryls...
June 27, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28687079/expression-and-function-of-phosphodiesterases-pdes-in-the-rat-urinary-bladder
#8
Xiaofei Zhu, Kui Zhai, Yue Mi, Guangju Ji
BACKGROUND: It has been shown that hosphodiesterases (PDEs) play an important role in mediating the smooth muscle tone of rat urinary bladder. However, the gene expression profiles of them were still unknown. METHODS: Urinary bladder Strips were obtained from both neonatal and adult Sprague-Dawley rats. RT-PCR/western blot and organ bath were used to measure the expression and function of PDEs. RESULTS: Adult rat urinary bladder expressed various PDE mRNA with the following rank order: PDE5A ≈ PDE9A ≈ PDE10A > PDE2A ≈ PDE4A ≈ PDE4D > PDE4B ≈ PDE3B ≈ PDE8B ≈ PDE7A ≈ PDE7B > PDE1A...
July 7, 2017: BMC Urology
https://www.readbyqxmd.com/read/28684234/roflumilast-treatment-inhibits-lung-carcinogenesis-in-benzo-a-pyrene-induced-murine-lung-cancer-model
#9
Chang Dong Yeo, Young Ae Kim, Hwa Young Lee, Jin Woo Kim, Seung Joon Kim, Sang Haak Lee, Young Kyoon Kim
Roflumilast, a potent and selective inhibitor of phosphodiesterase-4 (PDE4), has been used in treatment of COPD. PDE4 inhibitor is associated with inhibition of chronic airway inflammation, oxidative stress, and mesenchymal markers in B(a)P-induced lung tumors. The aim of this study was to assess whether roflumilast alone or added to inhaled budesonide might have dose-dependent inhibition on lung carcinogenesis induced by carcinogen B(a)P in mice. Female A/J mice were given a single dose of benzo(a)pyrene. Administration of roflumilast (1mg/kg or 5mg/kg) via oral gavage and aerosolized budesonide (2...
July 3, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28681318/phosphodiesterase-4-inhibitor-therapies-for-atopic-dermatitis-progress-and-outlook
#10
Jusleen Ahluwalia, Jeremy Udkoff, Andrea Waldman, Jenna Borok, Lawrence F Eichenfield
Phosphodiesterase 4 (PDE4) is a cyclic AMP degrading enzyme in leukocytes. Several decades ago, increased PDE activity was demonstrated in patients with atopic dermatitis (AD). Currently, several PDE4 inhibitors in both topical and oral formulation have been developed to target the inflammatory cascade of AD. This review shows the pathogenic rationale behind these inhibitors, and discusses multiple PDE4 inhibitors that are under evaluation or in the market. PDE4 inhibitors may be considered as favorable agents in the repertoire of current interventions for AD...
July 5, 2017: Drugs
https://www.readbyqxmd.com/read/28680572/pulmonary-arterial-hypertension-in-the-usa-an-epidemiological-study-in-a-large-insured-pediatric-population
#11
Lin Li, Susan Jick, Stefanie Breitenstein, Gemzel Hernandez, Alexander Michel, David Vizcaya
Pulmonary arterial hypertension (PAH) is rare in children and few data are available in a pediatric general population. This study aims to calculate the annual incidence and prevalence of PAH and to describe these children in a large US population of patients aged under 18 years. Using the US MarketScan claims database we identified 695 children with PAH in 2010-2013. We calculated annual incidence rates and prevalence overall, by age and PAH type (idiopathic and non-idiopathic) using Byar's method. We also described characteristics, co-morbidities, treatment patterns, and diagnostic procedures for these children...
March 2017: Pulmonary Circulation
https://www.readbyqxmd.com/read/28677661/a-novel-therapeutic-approach-in-the-treatment-of-pulmonary-arterial-hypertension-allium-ursinum-liophylisate-alleviates-symptoms-comparably-to-sildenafil
#12
Mariann Bombicz, Daniel Priksz, Balazs Varga, Andrea Kurucz, Attila Kertész, Akos Takacs, Aniko Posa, Rita Kiss, Zoltan Szilvassy, Bela Juhasz
Right-sided heart failure-often caused by elevated pulmonary arterial pressure-is a chronic and progressive condition with particularly high mortality rates. Recent studies and our current findings suggest that components of Wild garlic (Allium ursinum, AU) may play a role in reducing blood pressure, inhibiting angiotensin-converting enzyme (ACE), as well as improving right ventricle function in rabbit models with heart failure. We hypothesize that AU may mitigate cardiovascular damage caused by pulmonary arterial hypertension (PAH) and has value in the supplementary treatment of the complications of the disease...
July 4, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28668106/atopic-dermatitis-treatment-current-state-of-the-art-and-emerging-therapies
#13
Jonathan I Silverberg
BACKGROUND: Atopic dermatitis (AD) can be debilitating and often requires the use of combination topical and systemic therapy to achieve adequate disease control. METHODS: A non-systematic review was performed of current state of the art and emerging therapies for AD. RESULTS: There are a number of topical agents approved by the U.S. Food and Drug Administration (FDA) for the treatment of AD and multiple nonapproved systemic agents that are used off label for the treatment of AD...
July 1, 2017: Allergy and Asthma Proceedings:
https://www.readbyqxmd.com/read/28654711/addressing-the-immunopathogenesis-of-atopic-dermatitis-advances-in-topical-and-systemic-treatment
#14
Lawrence F Eichenfield, Linda F Stein Gold
Several immunologic mediators-phosphodiesterase (PDE), interleukin (IL), small molecules, and Janus kinase-have been implicated in the pathogenesis of atopic dermatitis, and evidence has shown that blocking these mediators can help modify the disease process. Several new topical medications have been developed that target the enzyme PDE; crisaborole was recently approved by the US Food and Drug Administration (FDA) for the treatment of atopic dermatitis, and phase II studies have been completed on OPA-15406...
March 2017: Seminars in Cutaneous Medicine and Surgery
https://www.readbyqxmd.com/read/28651653/influence-of-nitric-oxide-and-phosphodiesterases-during-in-vitro-maturation-of-bovine-oocytes-on-meiotic-resumption-and-embryo-production
#15
Ramon Cesar Botigelli, Katia Lancellotti Schwarz, Fabiane Gilli Zaffalon, Maite Del Collado, Fernanda Cavallari Castro, Hugo Fernandes, Claudia Lima Verde Leal
This study aimed to examine the effects of nitric oxide (NO) and different phosphodiesterase (PDE) families on meiosis resumption, nucleotides levels and embryo production. Experiment I, COCs were matured in vitro with the NO donor S-nitroso-N-acetylpenicillamine (SNAP) associated or not with the soluble guanylate cyclase (sGC) inhibitor 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ), meiotic resumption and nucleotides levels were assessed. SNAP delayed germinal vesicle breakdown (GVBD) (53.4 ± 1.2 versus 78...
June 27, 2017: Zygote: the Biology of Gametes and Early Embryos
https://www.readbyqxmd.com/read/28651482/modulation-of-some-markers-of-erectile-dysfunction-and-malonaldehyde-levels-in-isolated-rat-penile-tissue-with-unripe-and-ripe-plantain-peels-identification-of-the-constituents-of-the-plants-using-hplc
#16
Ganiyu Oboh, Adedayo Oluwaseun Ademiluyi, Sunday Idowu Oyeleye, Tosin Abiola Olasehinde, Aline Augusti Boligon
CONTEXT: Plantain fruit pulp has been used as a natural remedy to manage erectile dysfunction (ED) in traditional medicine. However, the potency of the peel has not been examined with respect to ED management. OBJECTIVE: This study investigated and compared the inhibitory potential of unripe (UPP) and ripe (RPP) plantain peels on some enzymes associated with ED and Fe(2+)-induced oxidative stress in albino rat penile homogenate in vitro. MATERIALS AND METHOD: Aqueous extract of the peels was prepared and the effect on phosphodiesterase-5 (PDE-5), arginase, acetylcholinesterase (AChE), angiotensin-I converting enzyme (ACE) and Fe(2+)-induced malonyladehyde in isolated albino rat penile homogenate were investigated...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28650427/roflumilast-reverses-polymicrobial-sepsis-induced-liver-damage-by-inhibiting-inflammation-in-mice
#17
Hongfang Feng, Jiajia Chen, Haitao Wang, Yufang Cheng, Zhengqiang Zou, Qiuping Zhong, Jiangping Xu
Sepsis is a life-threatening syndrome accompanied by an overwhelming inflammatory response and organ dysfunction. Selective targeting of phosphodiesterase 4 (PDE4) is currently being investigated as an effective therapeutic approach for inflammation-associated diseases. Roflumilast is a selective PDE4 inhibitor, used for the treatment of severe chronic obstructive pulmonary disease in clinic. However, its role in the treatment of sepsis-induced liver damage remains unclear. In the present study, we evaluated the effects of roflumilast in mice with cecal ligation and puncture-induced sepsis, and investigated the underlying mechanism...
June 26, 2017: Laboratory Investigation; a Journal of Technical Methods and Pathology
https://www.readbyqxmd.com/read/28649129/c33-s-a-novel-pde9a-inhibitor-protects-against-rat-cardiac-hypertrophy-through-upregulating-cgmp-signaling
#18
Pan-Xia Wang, Zhuo-Ming Li, Si-Dong Cai, Jing-Yan Li, Ping He, Yi Huang, Guo-Shuai Feng, Hai-Bin Luo, Shao-Rui Chen, Pei-Qing Liu
Phosphodiesterase-9A (PDE9A) expression is upregulated during cardiac hypertrophy and heart failure. Accumulating evidence suggests that PDE9A might be a promising therapeutic target for heart diseases. The present study sought to investigate the effects and underlying mechanisms of C33(S), a novel selective PDE9A inhibitor, on cardiac hypertrophy in vitro and in vivo. Treatment of neonatal rat cardiomyocytes (NRCMs) with PE (100 μmol/L) or ISO (1 μmol/L) induced cardiac hypertrophy characterized by significantly increased cell surface areas and increased expression of fetal genes (ANF and BNP)...
June 26, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28638635/crystal-structure-of-an-apremilast-ethanol-hemisolvate-hemihydrate-solvatomorph
#19
Yun-Deng Wu, Xiao-Hong Liu, Jian Xu, Si-Han Zhang, Kun Shen, Ling Sun, Yong-Mei He, Yan Ma, Ai-Hua Zhang
The title compound, C22H24N2O7S·0.5C2H5OH·0.5H2O {systematic name: (S)-4-acetamido-2-[1-(3-eth-oxy-4-meth-oxy-phen-yl)-2-(methyl-sulfon-yl)eth-yl]iso-indo-line-1,3-dione ethanol hemisolvate hemihydrate}, is a novel solvatomorph of apremilast (AP), which is an inhibitor of phosphodiesterase 4 (PDE4) and is indicated for the treatment of adult patients with active psoriatic arthritis. The asymmetric unit contains one mol-ecule of AP and disordered mol-ecules of ethanol and water, both with half occupancy. The dihedral angle between the planes of the phenyl ring and the iso-indole ring is 67...
June 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28637505/human-lung-and-monocyte-derived-macrophages-differ-with-regard-to-the-effects-of-%C3%AE-2-adrenoceptor-agonists-on-cytokine-release
#20
Tatiana Victoni, Hélène Salvator, Charlotte Abrial, Marion Brollo, Luis Cristovão Sobrino Porto, Vincent Lagente, Emmanuel Naline, Stanislas Grassin-Delyle, Philippe Devillier
BACKGROUND: β2-adrenoceptor agonists have been shown to reduce the lipopolysaccharide (LPS)-induced cytokine release by human monocyte-derived macrophages (MDMs). We compare the expression of β2-adrenoceptors and the inhibitory effect of formoterol and salmeterol on the LPS-induced release of tumor necrosis factor (TNF)-α, interleukin (IL)-1β, IL-6 and a range of chemokines (CCL2, 3, 4, and IL-8) by human lung macrophages (LMs) and MDMs. METHODS: LMs were isolated from patients undergoing resection and MDMs were obtained from blood monocytes in the presence of GM-CSF...
June 21, 2017: Respiratory Research
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