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https://www.readbyqxmd.com/read/29148852/sildenafil-citrate-improves-the-delivery-and-anticancer-activity-of-doxorubicin-formulations-in-a-mouse-model-of-breast-cancer
#1
Khaled Greish, Maryam Fateel, Sara Abdelghany, Nanitha Rachel, Houman Alimoradi, Moiz Bakhiet, Ahmed Alsaie
Sildenafil is an approved drug for the treatment of erectile dysfunction. The drug exerts its action through the relaxation of smooth muscles and the modulation of vascular endothelial permeability. In this work, we tested whether the aforementioned effects of Sildenafil on tumor vasculatures could result in an improvement of anticancer drug concentration in tumor tissues, and hence improve its anticancer effect. Sildenafil when added to doxorubicin showed synergistic anticancer activity against 4T1 breast cancer cells in vitro...
November 17, 2017: Journal of Drug Targeting
https://www.readbyqxmd.com/read/29141888/lung-cancer-associated-pulmonary-hypertension-role-of-microenvironmental-inflammation-based-on-tumor-cell-immune-cell-cross-talk
#2
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, KRas(LA2) , and cRaf-BxB)...
November 15, 2017: Science Translational Medicine
https://www.readbyqxmd.com/read/29136854/disperse-magnetic-solid-phase-microextraction-and-surface-enhanced-raman-scattering-dis-mspme-sers-for-the-rapid-detection-of-trace-illegally-chemicals
#3
Shihua Yu, Zhigang Liu, Weixian Wang, Li Jin, Weiqing Xu, Yuqing Wu
The technique of solid phase micro-extraction (SPME) is an important method for sample pretreatment in analytical chemistry, especially for the analysis in micro-systems. Surface enhanced Raman scattering (SERS) is an ultra-sensitive and fast detection technique. Both are particularly important in qualitative analysis of trace amount of substance. In this study, combining the magnetic nanoparticles with magnetic SPME device, we develop a high efficient new pretreatment method named as disperse magnetic solid phase micro-extraction (Dis-MSPME)...
February 1, 2018: Talanta
https://www.readbyqxmd.com/read/29136555/non-targeted-metabolomics-guided-sildenafil-metabolism-study-in-human-liver-microsomes
#4
Ju-Hyun Kim, Jun Hyun Jo, Kyung-Ah Seo, Hayoung Hwang, Hye Suk Lee, Sangkyu Lee
Metabolomics combined with high-resolution mass spectrometry (HR-MS) and multivariate data analysis has broad applications in the study of xenobiotic metabolism. Although information about xenobiotic metabolism is essential to understand toxic mechanisms, pharmacokinetic parameters and excretion pathways, it is limited to predict all generated metabolites in biological fluids. Here, we revisited sildenafil metabolism in human liver microsomes using a metabolomics approach to achieve a global picture of sildenafil phase 1 metabolism...
November 7, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29135645/phosphodiesterase-type-5-inhibitors-sport-and-doping
#5
Luigi Di Luigi, Massimiliano Sansone, Andrea Sansone, Roberta Ceci, Guglielmo Duranti, Paolo Borrione, Clara Crescioli, Paolo Sgrò, Stefania Sabatini
Phosphodiesterase type 5 inhibitors (PDE5i) (e.g., sildenafil, tadalafil, vardenafil, and avanafil) are drugs commonly used to treat erectile dysfunction, pulmonary arterial hypertension, and benign prostatic hyperplasia. PDE5i are not prohibited by the World Anti-Doping Agency (WADA) but are alleged to be frequently misused by healthy athletes to improve sporting performance. In vitro and in vivo studies have reported various effects of PDE5i on cardiovascular, muscular, metabolic, and neuroendocrine systems and the potential, therefore, to enhance performance of healthy athletes during training and competition...
November 2017: Current Sports Medicine Reports
https://www.readbyqxmd.com/read/29134978/testicular-and-epididymal-histology-of-rats-chronically-administered-high-doses-of-phosphodiesterase-5-inhibitors-and-tramadol
#6
Victor U Nna, Augustine L Udefa, Emmanuel O Ofutet, Eme O Osim
Testicular oxidative stress, endocrine disruption and abnormal spermatogenesis in rats exposed to high doses ofphosphodiesterase-5 inhibitors (PDE5i) and opioids, with poor reversibility following withdrawal of treatment had beenreported. In this study, we examined the histopathological effects of high doses of sildenafil, tadalafil, tramadol andsildenafil+tramadol on the testes and epididymis of rats. Seventy male rats (180 - 200 g b.w) were assigned to one of fivegroups (n = 14), namely; A: control (0.2 mL normal saline), B: sildenafil (1 mg/100g b...
June 30, 2017: Nigerian Journal of Physiological Sciences: Official Publication of the Physiological Society of Nigeria
https://www.readbyqxmd.com/read/29134487/sildenafil-citrate-use-in-addis-ababa-characteristics-of-users-and-pharmacists-dispensing-practices
#7
Dawit Teshome Gebregeorgise, Yajeb Melesse Belay, Sofia Kälvemark Sporrong
Background Studies have reported misuse of sildenafil citrate for recreational purpose, not least by healthy young men. This is becoming a major concern, for medical and other reasons. Objective The aim of this study was to document the characteristics of sildenafil citrate users and to explore the dispensing practices of the medicine in selected community pharmacies in Addis Ababa, Ethiopia. Setting Data was collected in community pharmacies in Addis Ababa, Ethiopia. Method A survey, using a self-administrated questionnaire, was conducted among customers who purchased sildenafil citrate from community pharmacies...
November 14, 2017: International Journal of Clinical Pharmacy
https://www.readbyqxmd.com/read/29132113/fluorometric-detection-of-protein-ligand-engagement-the-case-of-phosphodiesterase5
#8
Giulia Di Rocco, Ilaria Martinelli, Salvatore Pacifico, Remo Guerrini, Elena Cichero, Paola Fossa, Silvia Franchini, Silvia Cardarelli, Mauro Giorgi, Marco Sola, Glauco Ponterini
Phosphodiesterases (PDEs) regulate the intracellular levels of cAMP and cGMP. The great clinical success of the PDE5 inhibitors, Sildenafil (Viagra), Vardenafil (Levitra) and Tadalafil (Cialis) has led to an increasing interest for this class of enzymes. Recent studies have shown a correlation between tumor growth and PDE5 overexpression, making PDE5-selective inhibitors promising candidates for cancer treatment. The search for such inhibitors rests today on radioactive assays. In this work, we exploit the conserved catalytic domain of the enzyme and propose a faster and safer method for detecting the binding of ligands and evaluate their affinities...
November 10, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29131022/an-echocardiographic-screening-program-helps-to-identify-pulmonary-hypertension-in-extremely-low-birthweight-infants-with-and-without-bronchopulmonary-dysplasia-a-single-center-experience
#9
Katrin Mehler, Floris E Udink Ten Cate, Titus Keller, Ursula Bangen, Angela Kribs, André Oberthuer
BACKGROUND: Pulmonary hypertension (PH) affects 1 in 6 infants with a birthweight <1,000 g (extremely low birthweight; ELBW) and is frequently associated with bronchopulmonary dysplasia (BPD). If untreated, the mortality rates of the disease are high. OBJECTIVES: The aim of this study was to characterize risk factors for PH in ELBW infants and to describe the timing of onset of the disease by setting up a screening program. METHODS: ELBW infants treated at the Department of Neonatology (level III neonatal intensive care unit at the University of Cologne Medical Centre, Germany) between January 2010 and March 2015 were included...
November 8, 2017: Neonatology
https://www.readbyqxmd.com/read/29129998/changes-in-retinal-and-choroidal-vascular-blood-flow-after-oral-sildenafil-an-optical-coherence-tomography-angiography-study
#10
David Berrones, Guillermo Salcedo-Villanueva, Virgilio Morales-Cantón, Raul Velez-Montoya
Purpose: To describe changes in the retina and choroidal flow by optical coherence tomography angiography (OCT-A) after a single dose of oral sildenafil. Method: A case-control study. Patients in the study group received 50 mg of oral sildenafil. Patients in the control group received a sham pill. Retinal and choroidal images were obtained at baseline (before pill ingestion) and 1 hour after ingestion. Central macular and choroidal thickness, choroidal and outer retina flow, and the retinal and choroidal vascular density were compared using a Mann-Whitney U test...
2017: Journal of Ophthalmology
https://www.readbyqxmd.com/read/29124030/large-atrial-septal-defect-closure-in-a-patient-with-severe-pulmonary-arterial-hypertension
#11
Supomo Supomo, Anggoro Budi Hartopo, Dyah Wulan Anggrahini, Handy Darmawan, Lucia Kris Dinarti
Patients with an atrial septal defect (ASD) and severe pulmonary arterial hypertension (PAH) are considered ineligible for defect closure surgery because of the risk of right ventricular decompensation and death after the operation. We report the case of a patient with large ASD and severe PAH who was able to undergo defect closure surgery successfully following long-term use of combined oral sildenafil and beraprost.
October 2017: Korean Journal of Thoracic and Cardiovascular Surgery
https://www.readbyqxmd.com/read/29118953/the-role-of-preoperative-sildenafil-therapy-in-controlling-of-postoperative-pulmonary-hypertension-in-children-with-ventricular-septal-defects
#12
Hamid Bigdelian, Mohsen Sedighi
Introduction: Most of the ventricular septal defects (VSD) are complicated with pulmonary arterial hypertension (PAH) which is the major cause of pulmonary hypertensive crisis and right ventricular failure. Methods: We reviewed clinical outcomes of 63 infants who underwent cardiac surgery and were divided into three groups. Control group (n=20) did not received sildenafil while group A (n = 22) received drug (0.3 mg/kg) before and after surgery. Group B (n=21) received drug at the initiation of surgery. Demographic data, preoperative and postoperative variables were compared among the patients...
2017: Journal of Cardiovascular and Thoracic Research
https://www.readbyqxmd.com/read/29113971/correction-to-2017-acc-aap-aha-health-policy-statement-on-opportunities-and-challenges-in-pediatric-drug-development-learning-from-sildenafil
#13
(no author information available yet)
No abstract text is available yet for this article.
November 2017: Circulation. Cardiovascular Quality and Outcomes
https://www.readbyqxmd.com/read/29110626/the-rationale-for-repurposing-sildenafil-as-an-adjuvant-to-lung-cancer-treatment
#14
Theodore Keats, Rhonda J Rosengren, John C Ashton
There is now a considerable body of evidence for sildenafil possessing anticancer properties. In this article we argue the case for testing sildenafil as a lung cancer therapy chemoadjuvant. Currently, lung cancer is a disease with insufficient treatment options, with only 20% of patients responding to systemic chemotherapy, and even incremental potential improvements should be explored. We review the literature concerning the biochemical, physiological and metabolic effects on cancer cells by sildenafil alone, and when combined with chemotherapeutic agents...
November 2, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29094165/phosphodiesterase-inhibitors-sildenafil-and-vardenafil-reduce-zebrafish-rod-photoreceptor-outer-segment-shedding
#15
Leah J Campbell, Abbie M Jensen
Purpose: The vertebrate rod photoreceptor undergoes daily growth and shedding to renew the rod outer segment (ROS), a modified cilium that contains the phototransduction machinery. It has been demonstrated that ROS shedding is regulated by the light-dark cycle; however, we do not yet have a satisfactory understanding of the molecular mechanisms that underlie this regulation. Given that phototransduction relies on the hydrolysis of cGMP via phosphodiesterase 6 (PDE6), we examined ROS growth and shedding in zebrafish treated with cGMP-specific PDE inhibitors...
November 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/29092891/sildenafil-is-associated-with-reduced-device-thrombosis-and-ischemic-stroke-despite-low-level-hemolysis-on-heart-mate-ii-support
#16
Omar Saeed, Sabarivinoth Rangasamy, Ibrahim Selevany, Shivank Madan, Jeremy Fertel, Ruth Eisenberg, Mohammad Aljoudi, Snehal R Patel, Julia Shin, Daniel B Sims, Morayma Reyes Gil, Daniel J Goldstein, Marvin J Slepian, Henny H Billett, Ulrich P Jorde
BACKGROUND: Persistent low-level hemolysis (LLH) during continuous-flow mechanical circulatory support is associated with subsequent thrombosis. Free hemoglobin from ongoing hemolysis scavenges nitric oxide (NO) to create an NO deficiency which can augment platelet function leading to a prothrombotic state. The phosphodiesterase-5 inhibitor, sildenafil, potentiates NO signaling to inhibit platelet function. Accordingly, we investigated the association of sildenafil administration and thrombotic events in patients with LLH during Heart Mate II support...
November 2017: Circulation. Heart Failure
https://www.readbyqxmd.com/read/29089445/novel-imaging-of-the-prostate-reveals-spontaneous-gland-contraction-and-excretory-duct-quiescence-together-with-different-drug-effects
#17
Robert Kügler, Andrea Mietens, Mathias Seidensticker, Sabine Tasch, Florian M Wagenlehner, Andre Kaschtanow, Yudy Tjahjono, Claudia U Tomczyk, Daniela Beyer, Gail P Risbridger, Betty Exintaris, Stuart J Ellem, Ralf Middendorff
Prostate carcinoma and benign prostate hyperplasia (BPH) with associated lower urinary tract symptoms (LUTS) are among the most prevalent and clinically relevant diseases in men. BPH is characterized by an enlargement of prostate tissue associated with increased tone of smooth muscle cells (SMCs) which surround the single glands composing the prostate. Secretions of the glands leave the prostate through local excretory ducts during the emission phase of ejaculation. Pharmacological treatment of BPH suggests different local drug targets based on reduction of prostate smooth muscle tone as the main effect and disturbed ejaculation as a common side effect...
October 31, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/29083021/sarcoidosis-associated-pulmonary-hypertension-treated-with-sildenafil-a-case-report
#18
Aneta Kacprzak, Monika Szturmowicz, Barbara Burakowska, Monika Franczuk, Jarosław Kober, Marcin Kurzyna, Michał Wilk, Sebastian Szmit, Adam Torbicki, Jan Kuś
Development of sarcoidosis-associated pulmonary hypertension (SAPH) significantly worsens prognosis in sarcoidosis patients. Unfortunately, there is no treatment of proven benefit for this condition. Medications used for treatment of pulmonary arterial hypertension are of great interest in this respect. Here, we report a case of a patient with severe SAPH treated with sildenafil. A significant, but only temporary improvement in functional status was observed, and the patient died of gradually progressing heart and respiratory failure while awaiting for lung transplantation...
October 30, 2017: Advances in Respiratory Medicine
https://www.readbyqxmd.com/read/29074293/relationship-between-asymmetric-dimethylarginine-nitrite-and-genetic-polymorphisms-impact-on-erectile-dysfunction-therapy
#19
Ana Maria Milanez Azevedo, Guilhermo Brites-Anselmi, Lucas Cezar Pinheiro, Vanessa de Almeida Belo, Fernanda Borchers Coeli-Lacchini, Carlos Augusto Fernandes Molina, Murilo Ferreira de Andrade, Silvio Tucci, Emilio Hirsch, Jose Eduardo Tanus-Santos, Riccardo Lacchini
Sildenafil is the most used treatment of erectile dysfunction, however a large part of patients do not respond to therapy. This drug enhances nitric oxide (NO) signaling, and therefore factors that alter NO production may impact this drug responsiveness. Asymmetric dimethylarginine (ADMA) is an endogenous inhibitor of all NO synthases, and is metabolized by Dimethylarginine Dimethilaminohydrolase (DDAH) 1 and 2. Here we aimed to assess the relationship between plasma levels of ADMA and nitrite (marker of nitric oxide production) with Sildenafil responsiveness...
October 23, 2017: Nitric Oxide: Biology and Chemistry
https://www.readbyqxmd.com/read/29067241/effect-of-phosphodiesterase-5-inhibitors-on-glycemic-control-in-person-with-type-2-diabetes-mellitus-a-systematic-review-and-meta-analysis
#20
Nalinee Poolsup, Naeti Suksomboon, Nandar Aung
Chronic use of phosphodiesterase-5 inhibitors (PDE-5i) has been shown to improve insulin action on muscle glucose uptake by the prolongation of nitric oxide (NO)/cyclic guanosine monophosphate (cGMP)/protein kinase (PKG) signalling. AIMS: As the effects of PDE-5i on glycemic control in person with type 2 diabetes mellitus (T2DM) have not been systematically explored, we conducted a meta-analysis of available randomized controlled trials (RCTs). METHODS: A literature search was performed through electronic databases including MEDLINE (Pubmed), The Cochrane Library, SCOPUS, Web of Science, CINAHL, www...
December 2016: Journal of Clinical & Translational Endocrinology
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