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PDE5 Inhibitors

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https://www.readbyqxmd.com/read/29438488/cardioprotection-by-ischemic-postconditioning-and-cgmp-elevating-agents-involves-cardiomyocyte-nitric-oxide-sensitive-guanylyl-cyclase
#1
Sandra Frankenreiter, Dieter Groneberg, Anna Kuret, Thomas Krieg, Peter Ruth, Andreas Friebe, Robert Lukowski
Aims: It has been suggested that the nitric oxide-sensitive guanylyl cyclase (NO-GC)/cGMP-dependent signaling pathway affords protection against cardiac damage during acute myocardial infarction (AMI). It is, however, not clear whether the NO-GC/cGMP system confers its favorable effects through a mechanism located in cardiomyocytes (CMs). The aim of this study was to evaluate the infarct-limiting effects of the endogenous NO-GC in CMs in vivo. Methods and Results: Ischemia/reperfusion (I/R) injury was evaluated in mice with a cardiomyocyte-specific deletion of NO-GC (CM NO-GC KO) and in control siblings (CM NO-GC CTR) subjected to an in vivo model of AMI...
February 9, 2018: Cardiovascular Research
https://www.readbyqxmd.com/read/29438213/new-no-donor-ncx-1443-therapeutic-effects-on-pulmonary-hypertension-in-the-sad-mouse-model-of-sickle-cell-disease
#2
Shariq Abid, Kanny Kebe, Amal Houssaïni, Françoise Tomberli, Elisabeth Marcos, Emilie Bizard, Marielle Breau, Aurelien Parpaleix, Claire-Marie Tissot, Bernard Maitre, Larissa Lipskaia, Genevieve Derumeaux, Elena Bastia, Armand Mekontso-Dessap, Serge Adnot
Nitric oxide (NO) donors may be useful for treating pulmonary hypertension (PH) complicating sickle cell disease (SCD), as endogenous NO is inactivated by hemoglobin released by intravascular hemolysis. Here, we investigated the effects of the new NO donor NCX1443 on PH in transgenic SAD mice, which exhibit mild SCD without severe hemolytic anemia. In SAD and wild-type (WT) mice, the pulmonary pressure response to acute hypoxia was similar and was abolished by 100 mg/kg NCX1443. The level of PH was also similar in SAD and WT mice exposed to chronic hypoxia (9% O2) alone or with SU5416, and was similarly reduced by daily NCX1443 gavage...
February 8, 2018: Journal of Cardiovascular Pharmacology
https://www.readbyqxmd.com/read/29417353/perioperative-management-with-phosphodiesterase-type-5-inhibitor-and-prostaglandin-e1-for-moderate-portopulmonary-hypertension-following-adult-to-adult-living-donor-liver-transplantation-a-case-report
#3
Takashi Onoe, Asuka Tanaka, Kohei Ishiyama, Kentaro Ide, Hirotaka Tashiro, Hideki Ohdan
BACKGROUND: Portopulmonary hypertension (PPH) is a relatively rare but well-recognized complication of end-stage liver disease. Moderate or severe PPH (mean pulmonary artery pressure [mPAP] ≥ 35 mmHg) is usually a contraindication for liver transplantation due to high operation-related mortality. Here, we report on a patient with moderate PPH whose condition was successfully managed with a phosphodiesterase type 5 (PDE5) inhibitor (tadalafil) and prostaglandin E1, who experienced rapid improvement of PPH after living-donor liver transplantation (LDLT)...
February 7, 2018: Surgical Case Reports
https://www.readbyqxmd.com/read/29395941/vardenafil-inhibiting-parasympathetic-function-of-tracheal-smooth-muscle
#4
Fei-Peng Lee, Pin-Zhir Chao, Hsing-Won Wang
BACKGROUND: Levitra, a phosphodiesterase-5 (PDE5) inhibitor, is the trade name of vardenafil. Nowadays, it is applied to treatment of erectile dysfunction. PDE5 inhibitors are employed to induce dilatation of the vascular smooth muscle. The effect of Levitra on impotency is well known; however, its effect on the tracheal smooth muscle has rarely been explored. When administered for sexual symptoms via oral intake or inhalation, Levitra might affect the trachea. METHODS: This study assessed the effects of Levitra on isolated rat tracheal smooth muscle by examining its effect on resting tension of tracheal smooth muscle, contraction caused by 10-6 M methacholine as a parasympathetic mimetic, and electrically induced tracheal smooth muscle contractions...
January 27, 2018: Journal of the Chinese Medical Association: JCMA
https://www.readbyqxmd.com/read/29386424/phosphodiesterase-9-pde9-regulate-bovine-tracheal-smooth-muscle-relaxation
#5
Tsuyoshi Tajima, Tamami Shinoda, Norimoto Urakawa, Kazumasa Shimizu, Takeharu Kaneda
The present study was designed to clarify phosphodiesterase 9 (PDE9) expression in bovine tracheal smooth muscle tissue, and to elucidate that PDE9 may contribute to the regulation of airway relaxation. PDE9 mRNA expression was detected in bovine tracheal smooth muscle. Sodium nitroprusside (an NO donor) and BAY 73-6691 (a selective PDE9 inhibitor) reduced high K+- and carbachol-induced contraction. BAY 73-6691 relaxed tracheal tissue on the same level with vardenafil (a selective PDE5 inhibitor). These results support our hypothesis that PDE9 plays functional role in the tracheal smooth muscle relaxation...
January 30, 2018: Journal of Veterinary Medical Science
https://www.readbyqxmd.com/read/29376615/-current-approaches-to-conservative-treatment-of-men-with-concomitant-benign-prostatic-hyperplasia-and-erectile-dysfunction
#6
A A Kamalov, A M Takhirzade
The article reviews the results of various conservative treatments for concomitant benign prostatic hyperplasia (BPH) and erectile dysfunction (ED). Phosphodiesterase type 5 (PDE5) inhibitors remain the first-line therapy for this category of patients taking into account their positive effect on both ED and BPH. The preferred treatment scheme includes PDE-5 inhibitor co-administered with 1-adrenoblocker. However, other combination treatments are considered promising, for example, a PDE-5 inhibitor with a 5-reductase inhibitor or a three-component treatment regimen: 1-adrenoblocker + 5-reductase inhibitor + PDE-5 inhibitor...
December 2017: Urologii︠a︡
https://www.readbyqxmd.com/read/29375047/effects-of-tadalafil-pde5-inhibitor-and-roflumilast-pde4-inhibitor-on-airway-reactivity-and-markers-of-inflammation-in-ovalbumin-induced-airway-hyperresponsiveness-in-guinea-pigs
#7
J Mokry, A Urbanova, I Medvedova, M Kertys, P Mikolka, P Kosutova, D Mokra
Selective phosphodiesterase (PDE) 4 inhibitors have recently been introduced into the therapy of chronic obstructive pulmonary disease. However, suppression of airway reactivity and eosinophilic inflammation by increased intracellular cAMP could be beneficial in bronchial asthma as well. PDE5 inhibitors are used for the therapy of erectile dysfunction, pulmonary hypertension, and other cardiovascular diseases, but an expression of PDE5 in several immune cells suggests its perspectives in inflammation, as well...
October 2017: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
https://www.readbyqxmd.com/read/29364918/riociguat-versus-sildenafil-on-hypoxic-pulmonary-vasoconstriction-and-ventilation-perfusion-matching
#8
Virginia Chamorro, Daniel Morales-Cano, Javier Milara, Bianca Barreira, Laura Moreno, María Callejo, Gema Mondejar-Parreño, Sergio Esquivel-Ruiz, Julio Cortijo, Ángel Cogolludo, Joan A Barberá, Francisco Perez-Vizcaino
INTRODUCTION: Current treatment with vasodilators for pulmonary hypertension associated with respiratory diseases is limited by their inhibitory effect on hypoxic pulmonary vasoconstriction (HPV) and uncoupling effects on ventilation-perfusion (V'/Q'). Hypoxia is also a well-known modulator of the nitric oxide (NO) pathway, and may therefore differentially affect the responses to phosphodiesterase 5 (PDE5) inhibitors and soluble guanylyl cyclase (sGC) stimulators. So far, the effects of the sGC stimulator riociguat on HPV have been poorly characterized...
2018: PloS One
https://www.readbyqxmd.com/read/29360833/the-role-of-cgmp-as-a-mediator-of-lipolysis-in-bovine-oocytes-and-its-effects-on-embryo-development-and-cryopreservation
#9
Kátia R L Schwarz, Fernanda C de Castro, Letícia Schefer, Ramon C Botigelli, Daniela M Paschoal, Hugo Fernandes, Cláudia L V Leal
This study aimed to determine the influence of cyclic guanosine 3'5'-monophosphate (cGMP) and cGMP-dependent kinase (PKG) during in vitro maturation (IVM) on lipolysis-related parameters in bovine cumulus-oocyte complexes (COCs), and on embryo development and cryosurvival. COCs were matured with cGMP/PKG modulators and assessed for metaphase II rates (MII), cGMP levels, lipid content in oocytes (OO), transcript abundance for genes involved in lipolysis (ATGL) and lipid droplets (PLIN2) in cumulus cells (CC) and OO, and presence of phosphorylated (active) hormone sensitive lipase (HSLser563) in OO...
2018: PloS One
https://www.readbyqxmd.com/read/29337269/inhibitors-of-phosphodiesterases-in-the-treatment-of-cough
#10
REVIEW
Juraj Mokry, Anna Urbanova, Martin Kertys, Daniela Mokra
A group of 11 enzyme families of metalophosphohydrolases called phosphodiesterases (PDEs) is responsible for a hydrolysis of intracellular cAMP and cGMP. Xanthine derivatives (methylxanthines) inhibit PDEs without selective action on their single isoforms and lead to many pharmacological effects, e.g. bronchodilation, anti-inflammatory and immunomodulating effects, and thus they can modulate the cough reflex. Contrary, selective PDE inhibitors have been developed to inhibit PDE isoforms with different pharmacological effects based on their tissue expression...
January 11, 2018: Respiratory Physiology & Neurobiology
https://www.readbyqxmd.com/read/29301746/cyclic-gmp-elevating-agents-suppress-polyposis-in-apc-min-mice-by-targeting-the-preneoplastic-epithelium
#11
Sarah K Sharman, Bianca N Islam, Yali Hou, Nagendra Singh, Franklin G Berger, Subbaramiah Sridhar, Wonsuk Yoo, Darren D Browning
The cGMP signaling axis has been implicated in the suppression of intestinal cancers but the inhibitory mechanism and the extent to which this pathway can be targeted remains poorly understood. The present study has tested the effect of cGMP-elevating agents on tumorigenesis in the ApcMin/+ mouse model of intestinal cancer. Treatment of ApcMin/+ mice with the receptor guanylyl-cyclase C (GCC) agonist linaclotide, or the phosphodiesterase-5 (PDE5) inhibitor sildenafil, significantly reduced the number of polyps per mouse (67% and 50% respectively)...
January 4, 2018: Cancer Prevention Research
https://www.readbyqxmd.com/read/29283882/sildenafil-a-phosphodiesterase-5-inhibitor-offers-protection-against-carbon-tetrachloride-induced-hepatotoxicity-in-rat
#12
Olorunfemi R Molehin, Anne A Adeyanju, Stephen A Adefegha, Oluwasanmi O Aina, Blessing A Afolabi, Ayorinde O Olowoyeye, Jesutomi A Oyediran, Opeyemi R Oladiran
BACKGROUND: Elevation of phosphodiesterase-5 (PDE5) activity converts cyclic guanosine monophosphate (cGMP) to 5'-GMP, a mechanism that could be associated with drug-mediated hepatotoxicity. This study investigated whether selective inhibition of PDE5 by sildenafil could offer protection against hepatotoxicity induced by carbon tetrachloride (CCl4). METHODS: CCl4 (0.5 mL/kg) was administered intraperitoneally to induce hepatotoxicity. The control group received normal saline...
December 28, 2017: Journal of Basic and Clinical Physiology and Pharmacology
https://www.readbyqxmd.com/read/29277372/effects-of-chlorogenic-acid-on-carbachol-induced-contraction-of-mouse-urinary-bladder
#13
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/29245915/curcumin-interacts-with-sildenafil-to-kill-gi-tumor-cells-via-endoplasmic-reticulum-stress-and-reactive-oxygen-nitrogen-species
#14
Jane L Roberts, Andrew Poklepovic, Laurence Booth
The present studies focused on the ability of the phosphodiesterase 5 (PDE5) inhibitor sildenafil to enhance the anti-cancer properties of clinically relevant concentrations of the dietary diarylheptanoid curcumin. In gastrointestinal tumor cells, sildenafil and curcumin interacted in a greater than additive fashion to kill. Inhibition of the extrinsic apoptotic pathway suppressed killing by ∼50%, as did blockade of the intrinsic apoptotic pathway. Sildenafil and curcumin reduced mTORC1 and mTORC2 activity and increased Beclin1 levels and the numbers of autophagosomes and autolysosomes in cells in a PERK-eIF2α-dependent fashion...
November 21, 2017: Oncotarget
https://www.readbyqxmd.com/read/29220595/dose-dependent-effects-of-tadalafil-and-roflumilast-on-ovalbumin-induced-airway-hyperresponsiveness-in-guinea-pigs
#15
Anna Urbanova, Ivana Medvedova, Martin Kertys, Pavol Mikolka, Petra Kosutova, Daniela Mokra, Juraj Mokrý
INTRODUCTION: Chronic obstructive diseases of airways associated with cough and/or airway smooth muscle hyperresponsiveness are usually treated with bronchodilating and anti-inflammatory drugs. Recently, selective phosphodiesterase (PDE) 4 inhibitors have been introduced into the therapy of chronic obstructive pulmonary disease. Several studies have demonstrated their ability to influence the airway reactivity and eosinophilic inflammation by increasing the intracellular cAMP concentrations also in bronchial asthma...
December 8, 2017: Experimental Lung Research
https://www.readbyqxmd.com/read/29194814/how-sildenafil-viagra%C3%A2-may-cause-melanoma-a-histopathologic-study-providing-a-potential-physiological-etiopathological-mechanism
#16
W Clark Lambert, Muriel W Lambert, Christina M Ring, Claude E Gagna, Jose D Espinal-Mariotte, Robert A Schwartz
The potential role of phosphodiesterase type 5 inhibitors (PDE5-Is) sildenafil (Viagra® ), vardenafil (Levitra® ), and tadalafil (Cialis® ) in development of malignant melanoma is controversial. Four observational studies have examined the association of PDE5-Is) and melanoma (1-4). While a conclusion regarding causality is challenging, the biological basis for an association between PDE5-I exposure and melanoma remains compelling. Melanoma lines expressing the BRAF oncogene downregulate PDE5, leading to vasodilation, invasion and metastasis of melanoma cells (5)...
December 1, 2017: Journal of the European Academy of Dermatology and Venereology: JEADV
https://www.readbyqxmd.com/read/29175000/cyclic-nucleotide-signaling-changes-associated-with-normal-aging-and-age-related-diseases-of-the-brain
#17
REVIEW
Michy P Kelly
Deficits in brain function that are associated with aging and age-related diseases benefit very little from currently available therapies, suggesting a better understanding of the underlying molecular mechanisms is needed to develop improved drugs. Here, we review the literature to test the hypothesis that a break down in cyclic nucleotide signaling at the level of synthesis, execution, and/or degradation may contribute to these deficits. A number of findings have been reported in both the human and animal model literature that point to brain region-specific changes in Galphas (a...
January 2018: Cellular Signalling
https://www.readbyqxmd.com/read/29164831/udenafil-a-phosphodiesterase-5-inhibitor-reduces-body-weight-in-high-fat-fed-mice
#18
Seong Yul Ryu, Yoon Jung Choi, So Young Park, Jong Yeon Kim, Yong Dae Kim, Yong Woon Kim
PURPOSE: High-fat (HF) feeding induces hypothalamic leptin resistance via the activation of toll-like receptor 4 (TLR4). TLR4 deficiency confers resistance to diet-induced obesity. Udenafil, an anti-impotence drug, inhibits TLR4 in airway epithelial cells in vitro. In this study, we evaluated whether udenafil suppressed the hypothalamic expression of TLR4 and reduced body weight. MATERIALS AND METHODS: The hypothalamic expression of TLR4, phosphodiesterase 5 (PDE5), nuclear factor-κB (NF-κB), and myeloid differentiation primary response gene 88 (Myd88) was analyzed by real-time polymerase chain reaction after treating mice for 2 days with udenafil (0, 12, 120, or 600 μg/d)...
November 16, 2017: World Journal of Men's Health
https://www.readbyqxmd.com/read/29151951/potential-synergistic-effect-of-phosphodiesterase-inhibitors-with-chemotherapy-in-lung-cancer
#19
Kalliopi Domvri, Konstantinos Zarogoulidis, Nikolaos Zogas, Paul Zarogoulidis, Savvas Petanidis, Konstantinos Porpodis, Efrosini Kioseoglou, Wolfgang Hohenforst-Schmidt
Purpose: Lung cancer remains the leading cause of cancer-related deaths worldwide and novel therapeutic approaches targeting crucial pathways are urgently needed to improve its treatment. Differentiation-based therapeutics (Methylxanthines) and phosphodiesterase inhibitors (type 4 and 5), have been implicated in cancer treatment. Our objectives were to capture any potential anti-tumor effect of these drug combinations with chemotherapeutic agents in vitro. Methods: Theophylline as Methylxanthines, Roflumilast as phosphodiesterase type 4 (PDE4) inhibitor and Sildenafil as phosphodiesterase type 5 (PDE5) inhibitor are the drugs that we combined with the chemotherapeutic agents (Docetaxel, Cisplatin and Carboplatin) in vitro...
2017: Journal of Cancer
https://www.readbyqxmd.com/read/29141888/lung-cancer-associated-pulmonary-hypertension-role-of-microenvironmental-inflammation-based-on-tumor-cell-immune-cell-cross-talk
#20
Soni Savai Pullamsetti, Baktybek Kojonazarov, Samantha Storn, Henning Gall, Ylia Salazar, Janine Wolf, Andreas Weigert, Nefertiti El-Nikhely, Hossein Ardeschir Ghofrani, Gabriele A Krombach, Ludger Fink, Stefan Gattenlöhner, Ulf R Rapp, Ralph Theo Schermuly, Friedrich Grimminger, Werner Seeger, Rajkumar Savai
Dyspnea is a frequent, devastating, and poorly understood symptom of advanced lung cancer. In our cohort, among 519 patients who underwent a computed tomography scan for the diagnosis of lung cancer, 250 had a mean pulmonary artery diameter of >28 mm, indicating pulmonary hypertension (PH). In human lung cancer tissue, we consistently observed increased vascular remodeling and perivascular inflammatory cell accumulation (macrophages/lymphocytes). Vascular remodeling, PH, and perivascular inflammatory cell accumulation were mimicked in three mouse models of lung cancer (LLC1, KRasLA2 , and cRaf-BxB)...
November 15, 2017: Science Translational Medicine
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