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PDE5 Inhibitors

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https://www.readbyqxmd.com/read/28088782/pde5-inhibitors-enhance-the-lethality-of-pemetrexed-sorafenib
#1
Laurence Booth, Jane L Roberts, Andrew Poklepovic, Paul Dent
The combination of pemetrexed and sorafenib has significant clinical activity against a wide variety of tumor types in patients and the present studies were performed to determine whether sildenafil enhances the killing potential of [pemetrexed + sorafenib]. In multiple genetically diverse lung cancer cell lines, sildenafil enhanced the lethality of [pemetrexed + sorafenib]. The three-drug combination reduced the activities of AKT, mTOR and STAT transcription factors; increased the activities of eIF2α and ULK-1; lowered the expression of MCL-1, BCL-XL, thioredoxin and SOD2; and increased the expression of Beclin1...
January 9, 2017: Oncotarget
https://www.readbyqxmd.com/read/28053948/recreational-use-of-phosphodiesterase-5-inhibitors-and-its-associated-factors-among-undergraduate-male-students-in-an-ethiopian-university-a-cross-sectional-study
#2
Eyob Alemayehu Gebreyohannes, Akshaya Srikanth Bhagavathula, Begashaw Melaku Gebresillassie, Yonas Getaye Tefera, Sewunet Admasu Belachew, Daniel Asfaw Erku
PURPOSE: To assess the prevalence of phosphodiesterase 5 (PDE5) inhibitor use and associated factors among University of Gondar undergraduate students. MATERIALS AND METHODS: An institution-based, cross-sectional study, using a survey questionnaire, was conducted from October to December 2015 to assess PDE5 inhibitor use and associated factors among male students at the University of Gondar. A Self-Esteem and Relationship questionnaire (14 items), an International Index of Erectile Function questionnaire (15 items) and a questionnaire on PDE5 inhibitor use (14 items) were included in the survey...
December 2016: World Journal of Men's Health
https://www.readbyqxmd.com/read/28042309/the-link-between-vascular-dysfunction-bladder-ischemia-and-aging-bladder-dysfunction
#3
REVIEW
Karl-Erik Andersson, Donna B Boedtkjer, Axel Forman
The vascular supply to the human bladder is derived mainly from the superior and inferior vesical arteries, the latter being directly connected to the internal iliac artery. Aging is associated with an impairment of blood vessel function and changes may occur in the vasculature at the molecular, cellular and functional level. Pelvic arterial insufficiency may play an important role in the development of bladder dysfunctions such as detrusor overactivity (DO) and the overactive bladder syndrome. Chronic ischemia-related bladder dysfunction may progress to bladder underactivity and it would be desirable to treat not only lower urinary tract symptoms (LUTS) induced by chronic ischemia, but also the progression of the morphological bladder changes...
January 2017: Therapeutic Advances in Urology
https://www.readbyqxmd.com/read/28025893/isoflavones-from-maclura-pomifera-structural-elucidation-and-in-silico-evaluation-of-their-interaction-with-pde5
#4
Giovanni Ribaudo, Tiziano Vendrame, Sergio Bova
While osajin and pomiferin are known for their anticancer, antibacterial and antidiabetic properties, scandenone and auriculasin have been proposed as anti-inflammatory and antinociceptive agents. Curiously, these two couples of molecules are, from a chemical point of view, structural isomers which can all be extracted from Maclura pomifera. Although previous works described, separately, the isolation in reasonable amounts of the sole osajin/pomiferin couple or of scandenone/auriculasin, we report the extraction and characterization using direct spectral and chromatographical comparison of the four compounds...
December 27, 2016: Natural Product Research
https://www.readbyqxmd.com/read/28018840/hand-impairment-in-systemic-sclerosis-various-manifestations-and-currently-available-treatment
#5
Amber Young, Rajaie Namas, Carole Dodge, Dinesh Khanna
Systemic sclerosis (SSc) is an autoimmune disease initially recognized by hand involvement due to characteristic Raynaud's phenomenon (RP), puffy hands, skin thickening, and contractures resembling claw deformities. SSc contributes to hand impairment through inflammatory arthritis, joint contractures, tendon friction rubs (TFRs), RP, digital ulcers (DU), puffy hands, skin sclerosis, acro-osteolysis, and calcinosis. These manifestations, which often co-exist, can contribute to difficulty with occupational activities and activities of daily living (ADL), which can result in impaired quality of life...
September 2016: Current Treatment Options in Rheumatology
https://www.readbyqxmd.com/read/28017777/the-cardioprotective-effect-of-sildenafil-is-mediated-by-the-activation-of-malate-dehydrogenase-and-an-increase-in-the-malate-aspartate-shuttle-in-cardiomyocytes
#6
Gevi Federica, Campolo Federica, Naro Fabio, Zolla Lello
Recent evidence has shown showed the cardioprotective effect of PDE5 inhibition in myocardial ischemia/reperfusion injury, heart failure and cardiac hypertrophy. To investigate the biochemical changes that occur during PDE5 inhibition in cardiac cells, this study assessed the metabolic profile of the HL1 cell line, a murine atrial cell line with adult cardiomyocyte properties. After one hour of treatment with sildenafil, glycolysis was moderately but selectively stimulated, unlike the pentose phosphate pathway and the Krebs cycle...
December 22, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/27981728/physicians-response-to-sexual-dysfunction-presented-by-a-younger-vs-an-older-adult
#7
Ateret Gewirtz-Meydan, Liat Ayalon
AIM: The aim of this study is to determine whether physicians have an age bias regarding sexual dysfunction presented by older vs. younger patients in terms of attributed diagnosis, etiology, proposed treatment and perceived prognosis. METHOD: An on-line survey consisting of one of two, randomly administered, case vignettes, which differed only by the age of the patient (28 or 78). In both cases, the patient was described as suffering from occasional erectile dysfunction with a clear psychosocial indication...
December 16, 2016: International Journal of Geriatric Psychiatry
https://www.readbyqxmd.com/read/27957675/the-importance-of-l-arginine-no-cgmp-pathway-in-tolerance-to-flunitrazepam-in-mice
#8
Sylwia Talarek, Joanna Listos, Jolanta Orzelska-Gorka, Malgorzata Jakobczuk, Jolanta Kotlinska, Grazyna Biala
The goal of the study was to investigate the effects of drugs modifying L-arginine:NO:cGMP pathway on the development of tolerance to flunitrazepam (FNZ)-induced motor impairment in mice. FNZ-induced motor incoordination was assessed on the 1st and 8th days of experiment, using the rotarod and chimney tests. It was found that (a) both a non-selective nitric oxide synthase (NOS) inhibitor: N (G)-nitro-L-arginine methyl ester (L-NAME) and an unselective neuronal NOS inhibitor: 7-nitroindazole (7-NI) inhibited the development of tolerance to the motor-impairing effects of FNZ in the rotarod and the chimney tests and (b) both a NO precursor: L-arginine and a selective inhibitor of phosphodiesterase 5 (PDE5): sildenafil did not affect the development of tolerance to FNZ-induced motor impairment in mice...
December 12, 2016: Neurotoxicity Research
https://www.readbyqxmd.com/read/27936591/impact-of-scaffold-exploration-on-novel-dual-acting-histone-deacetylases-and-phosphodiesterase-5-inhibitors-for-the-treatment-of-alzheimer-s-disease
#9
Juan A Sánchez-Arias, Obdulia Rabal, Mar Cuadrado-Tejedor, Irene de Miguel, Marta Pérez-González, Ana Ugarte, Elena Sáez, Maria Espelosin, Susana Ursua, Tan Haizhong, Wu Wei, Xu Musheng, Ana Garcia-Osta, Julen Oyarzabal
A novel systems therapeutics approach, involving simultaneous inhibition of phosphodiesterase 5 (PDE5) and histone deacetylase (HDAC), has been validated as a potentially novel therapeutic strategy for the treatment of Alzheimer's disease (AD). First-in-class dual inhibitors bearing a sildenafil core have been very recently reported, and the lead molecule 7 has proven this strategy in AD animal models. Because scaffolds may play a critical role in primary activities and ADME-Tox profiling as well as on intellectual property, we have explored alternative scaffolds (vardenafil- and tadalafil-based cores) and evaluated their impact on critical parameters such as primary activities, permeability, toxicity, and in vivo (pharmacokinetics and functional response in hippocampus) to identify a potential alternative lead molecule bearing a different chemotype for in vivo testing...
December 27, 2016: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/27928427/alprostadil-cream-in-the-treatment-of-erectile-dysfunction-clinical-evidence-and-experience
#10
REVIEW
Béatrice Cuzin
Erectile dysfunction (ED) is a very common disorder with a deep impact on quality of life on both patients and partners. Several options are available for treating ED: oral pharmacotherapy with phosphodiesterase 5 (PDE5) inhibitors currently represents the first-line option for many patients with ED. Alprostadil, a prostaglandin, has been marketed for many years as a urethral stick and an intracavernous injection for the treatment of ED. It is now available in the form of a cream (Vitaros/Virirec), a noninvasive treatment which combines an active drug (alprostadil, a synthetic prostaglandin E1) with a skin enhancer improving its local absorption directly at the site of action...
August 2016: Therapeutic Advances in Urology
https://www.readbyqxmd.com/read/27903966/pde5-inhibitors-enhance-the-lethality-of-pemetrexed-through-inhibition-of-multiple-chaperone-proteins-and-via-the-actions-of-cyclic-gmp-and-nitric-oxide
#11
Laurence Booth, Jane L Roberts, Andrew Poklepovic, Sarah Gordon, Paul Dent
Phosphodiesterase 5 (PDE5) inhibitors prevent the breakdown of cGMP that results in prolonged protein kinase G activation and the generation of nitric oxide. PDE5 inhibitors enhanced the anti-NSCLC cell effects of the NSCLC therapeutic pemetrexed. [Pemetrexed + sildenafil] activated an eIF2α - ATF4 - CHOP - Beclin1 pathway causing formation of toxic autophagosomes; activated a protective IRE1 - XBP-1 - chaperone induction pathway; and activated a toxic eIF2α - CHOP - DR4 / DR5 / CD95 induction pathway. [Pemetrexed + sildenafil] reduced the expression of c-FLIP-s, MCL-1 and BCL-XL that was blocked in a cell-type -dependent fashion by either over-expression of HSP90 / GRP78 / HSP70 / HSP27 or by blockade of eIF2α-CHOP signaling...
November 26, 2016: Oncotarget
https://www.readbyqxmd.com/read/27872007/the-role-of-pde5-inhibitors-and-the-no-cgmp-pathway-in-cancer
#12
REVIEW
Taylor C Peak, Ashley Richman, Serap Gur, Faysal A Yafi, Wayne J G Hellstrom
INTRODUCTION: Phosphodiesterase 5 (PDE5) inhibitors (PDE5i) have been used clinically for the treatment of erectile dysfunction, acting on the nitric oxide/cyclic guanosine monophosphate (NO/cGMP) signaling pathway. Simultaneously, researchers have elucidated the roles that this pathway plays in the regulation of cell proliferation, tumor development, and progression. As a result, our knowledge of PDE5i and cancer biology has expanded and provides an integration that holds great promise for some, but concern for others...
January 2016: Sexual Medicine Reviews
https://www.readbyqxmd.com/read/27855624/the-women-s-heart-insights-into-new-potential-targeted-therapy
#13
Daniele Gianfrilli, Ricardo Pofi, Tiziana Feola, Andrea Lenzi, Elisa Giannetta
Cardiovascular disease represents an increasing cause of death in women. The analysis of cardiovascular risk factors in women has not reached a consensus with respect to a specific and personalized treatment designed in pre-menopausal and post-menopausal phases. Clinically significant cardioprotective and antiremodeling effects were detected in animal and human study exploring chronic inhibition of Phosphodiesterase type 5 (PDE5). The relationship between heart, estrogens and PDE5 inhibitors (PDE5i) remains unclear...
November 18, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27843073/off-target-effect-of-sildenafil-on-postsurgical-erectile-dysfunction-alternate-pathways-and-localized-delivery-system
#14
Amirali Salmasi, Geun Taek Lee, Neal Patel, Ritu Goyal, Michael Dinizo, Young Suk Kwon, Part K Modi, Izak Faiena, Hee-Jin Kim, Nara Lee, Johanna L Hannan, Joachim Kohn, Isaac Yi Kim
INTRODUCTION: There is no consensus on the best oral phosphodiesterase type 5 inhibitor (PDE5I) for patients undergoing penile rehabilitation after surgical nerve injury. AIM: To determine the mechanism of PDE5I on cultured neuronal cells and the effectiveness of local drug delivery using nanospheres (NSPs) to sites of nerve injury in a rat model of bilateral cavernous nerve injury (BCNI). METHODS: The effects of sildenafil, tadalafil, and vardenafil on cyclic adenosine monophosphate, cyclic guanosine monophosphate, and cell survival after exposure to hypoxia and H2O2 were measured in PC12, SH-SY5Y, and NTERA-2 (NT2) cell cultures...
December 2016: Journal of Sexual Medicine
https://www.readbyqxmd.com/read/27836585/neuroprotective-effects-of-sildenafil-against-oxidative-stress-and-memory-dysfunction-in-mice-exposed-to-noise-stress
#15
Hu Erxidan Sikandaner, So Young Park, Min Jung Kim, Shi Nae Park, Dong Won Yang
Noise exposure has been well characterized as an environmental stressor, and is known to have auditory and non-auditory effects. Phosphodiesterase 5 (PDE5) inhibitors affect memory and hippocampus plasticity through various signaling cascades which are regulated by cGMP. In this study, we investigated the effects of sildenafil on memory deficiency, neuroprotection and oxidative stress in mice caused by chronic noise exposure. Mice were exposed to noise for 4h every day up to 14days at 110dB SPL of noise level...
February 15, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/27813474/-cyclic-nucleotide-phosphodiesterases-role-in-the-heart-and-therapeutic-perspectives
#16
Ibrahim Bedioune, Pierre Bobin, Sarah Karam, Marta Lindner, Delphine Mika, Patrick Lechêne, Jérôme Leroy, Rodolphe Fischmeister, Grégoire Vandecasteele
Cyclic nucleotide phosphodiesterases (PDEs) degrade the second messengers cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), thereby regulating multiple aspects of cardiac function. This highly diverse class of enzymes encoded by 21 genes encompasses 11 families that are not only responsible for the termination of cyclic nucleotide signalling, but are also involved in the generation of dynamic microdomains of cAMP and cGMP, controlling specific cell functions in response to various neurohormonal stimuli...
2016: Biologie Aujourd'hui
https://www.readbyqxmd.com/read/27785815/characterisation-of-pomegranate-juice-effects-on-human-corpus-cavernosum
#17
S Gur, B M Rezk, Z Y Abd Elmageed, P J Kadowitz, S C Sikka, W J G Hellstrom
Pomegranate (POM) juice may benefit the erectile process, but the scientific evidence is lacking. This study evaluates the molecular characterisation and confirmation of POM's action on human corpus cavernosum (HCC) obtained from patients (n = 16) undergoing penile prosthesis implantation. After phenylephrine contraction, the relaxant effects of POM with various inhibitors in the presence and absence of palmitic acid (PA)-induced acute oxidative stress were investigated. Electrical field stimulation (EFS)- and acetylcholine (ACh)-induced relaxation were performed using organ bath preparation...
October 26, 2016: Andrologia
https://www.readbyqxmd.com/read/27785443/dr-bang-ping-jiann-pde5-inhibitors-in-erectile-dysfunction
#18
Lucine M Gao
No abstract text is available yet for this article.
October 2016: Translational Andrology and Urology
https://www.readbyqxmd.com/read/27763717/additive-effects-of-the-rho-kinase-inhibitor-y-27632-and-vardenafil-on-relaxation-of-the-corpus-cavernosum-tissue-of-patients-with-erectile-dysfunction-and-clinical-phosphodiesterase-type-5-inhibitor-failure
#19
Pieter Uvin, Maarten Albersen, Ine Bollen, Maarten Falter, Emmanuel Weyne, Loes Linsen, Hanna Tinel, Peter Sandner, Trinity J Bivalacqua, Dirk J M K De Ridder, Frank Van der Aa, Bert Brône, Koenraad Van Renterghem
OBJECTIVES: To evaluate the expression of the Rho/Rho-associated protein kinase (ROCK) pathway in the corpus cavernosum of patients with severe erectile dysfunction (ED) compared with healthy human corpus cavernosum, and to test the functional effects of two Rho kinase inhibitors (RKIs) on erectile tissue of patients with severe ED, which did not respond to phosphodiesterase type 5 inhibitors (PDE5Is). PATIENTS AND METHODS: Human corpus cavernosum samples were obtained after consent from men undergoing penile prosthesis implantation (n = 7 for organ bath experiments, n = 17 for quantitative PCR [qPCR])...
October 20, 2016: BJU International
https://www.readbyqxmd.com/read/27747306/chemotherapeutic-efficacy-of-phosphodiesterase-inhibitors-in-chagasic-cardiomyopathy
#20
Jian-Jun Wen, Xianxiu Wan, John Thacker, Nisha Jain Garg
BACKGROUND: Chagasic cardiomyopathy (CCM) caused by Trypanosoma cruzi (Tc) infection is prevalent in Latin America and recognized as an emerging infectious heart disease in the US. The NO-cGMP-PKG1α pathway maintains cardiac homeostasis and inotropy and may be disturbed due to phosphodiesterase (PDE5) mediated cGMP catabolism in CCM. METHODS AND RESULTS: C57BL/6 mice were infected with Tc, and at the end of acute parasitemia (i.e. 45 days post-infection), treated with sildenafil (SIL, 1 mg/kg) twice per week for 3 weeks...
June 2016: JACC. Basic to Translational Science
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