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https://www.readbyqxmd.com/read/28821164/cape-gooseberry-physalis-peruviana-juice-as-a-modulator-agent-for-hepatocellular-carcinoma-linked-apoptosis-and-cell-cycle-arrest
#1
Hanaa A Hassan, Hanaa M Serag, Makwan S Qadir, Mohamed Fawzy Ramadan
BACKGROUND: Cape gooseberry (Physalis peruviana) fruit is highly nutritious with high content of health-promoting compounds including minerals, phenolic compounds, as well as vitamins A and C. Physalis peruviana fruits were used as mutagenic, antispasmodic, anticoagulant, and antileucemis agents. OBJECTIVE: The objective of the present work was to study the role of cape gooseberry juice (CG) as a natural modulator agent for adverse aspects associated with hepatocellular carcinoma (HCC)...
August 14, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28820912/impact-of-novel-palmitoylated-prolactin-releasing-peptide-analogs-on-metabolic-changes-in-mice-with-diet-induced-obesity
#2
Veronika Pražienková, Martina Holubová, Helena Pelantová, Martina Bugáňová, Zdenko Pirník, Barbora Mikulášková, Andrea Popelová, Miroslava Blechová, Martin Haluzík, Blanka Železná, Marek Kuzma, Jaroslav Kuneš, Lenka Maletínská
Analogs of anorexigenic neuropeptides, such as prolactin-releasing peptide (PrRP), have a potential as new anti-obesity drugs. In our previous study, palmitic acid attached to the N-terminus of PrRP enabled its central anorexigenic effects after peripheral administration. In this study, two linkers, γ-glutamic acid at Lys11 and a short, modified polyethylene glycol at the N-terminal Ser and/or Lys11, were applied for the palmitoylation of PrRP31 to improve its bioavailability. These analogs had a high affinity and activation ability to the PrRP receptor GPR10 and the neuropeptide FF2 receptor, as well as short-term anorexigenic effect similar to PrRP palmitoylated at the N-terminus...
2017: PloS One
https://www.readbyqxmd.com/read/28820269/reaction-phenotyping-to-assess-victim-drug-drug-interaction-risks
#3
Li Di
Reaction phenotyping provides critical information regarding the fraction metabolized (fm) of drug candidates. It has become increasingly important in drug discovery and development as it can be used to assess victim drug-drug interaction potential, guide structural modification to reduce fm, inform clinical study design, predict individual variability in pharmacokinetics, and evaluate the impact of genetic polymorphisms. Areas covered: The currently available in vitro and in vivo methods for reaction phenotyping are summarized along with their advantages, limitations and timings for application during the different stages of drug discovery and development...
August 18, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28819568/nebivolol-attenuates-neutrophil-lymphocyte-ratio-a-marker-of-subclinical-inflammation-in-hypertensive-patients
#4
Mazhar Hussain, Muhammad Saeed, Muhammad Zafar Majeed Babar, Moazzam Ali Atif, Lubna Akhtar
BACKGROUND: High value of neutrophil lymphocyte ratio (NLR) is a strong independent predictor and biomarker of ongoing vascular inflammation in various cardiovascular disorders. OBJECTIVE: The main focus of the study is to investigate the effect of nebivolol on NLR in mild to moderate hypertensive patients in comparison with metoprolol. In addition, BMI, blood pressure, TLC count, blood sugar, and lipid profile were also assayed before and after treatment. MATERIALS AND METHODS: In this 12-week prospective double-blinded randomized study, 120 patients with mild to moderate hypertension were randomly divided into two groups to prescribed daily dose of tab nebivolol 5-10 mg and metoprolol 50-100 mg, respectively, for 12 weeks...
2017: International Journal of Hypertension
https://www.readbyqxmd.com/read/28818532/myricetin-solid-lipid-nanoparticles-stability-assurance-from-system-preparation-to-site-of-action
#5
Dina M Gaber, Noha Nafee, Osama Y Abdallah
Myricetin - a natural flavonoid - has attracted a great interest due to its antioxidant and free-radical scavenging potential. However, its physicochemical instability critically impairs its dosage form design, evaluation and administration. In an attempt to protect from degradation, MYR was encapsulated into Gelucire-based solid lipid nanoparticles (SLNs). The impact of medium pH, processing temperature and different additives on the drug degradation either in free or nanoencapsulated form was assessed. MYR stability was further monitored in essential biorelevant fluids...
August 14, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28818482/drawbacks-of-the-use-of-cotrimoxazole-in-foreign-body-infections
#6
Cristina El Haj, Alba Ribera, Nuria Lloberas, Fe Tubau, Javier Ariza, Oscar Murillo
INTRODUCTION: The anti-staphylococcal efficacy of cotrimoxazole in the setting of difficult-to-treat infections seems to be compromised by large amounts of pus and devitalized tissue, and, therefore, high levels of thymidine. Our objective was to evaluate the activity of cotrimoxazole against a staphylococcal foreign-body infection experimental model, which also yields significant quantities of thymidine. MATERIAL AND METHODS: We used a rat tissue-cage model of infection (with high inherent thymidine levels) caused by a strain of methicillin-susceptible Staphylococcus aureus (MSSA; ATCC 29213)...
August 14, 2017: Enfermedades Infecciosas y Microbiología Clínica
https://www.readbyqxmd.com/read/28817968/destabilizing-the-interplay-between-mir-1275-and-igf2bps-by-tamarix-articulata-and-quercetin-in-hepatocellular-carcinoma
#7
Yasmin M Shaalan, H Handoussa, R A Youness, R A Assal, A H El-Khatib, M W Linscheid, H M El Tayebi, A I Abdelaziz
Insulin-like growth factor-2 binding proteins (IGF2BPs) are oncogenic RNA-binding proteins, highly up-regulated in HCC, and were recently validated as direct targets of the tumour suppressor miR-1275. It is worth noting that around 47% of FDA approved anticancer drugs are derived from plants. Modulation by miRNAs and their cellular signalling cascades could constitute new pathways by which these phytochemicals exert their effects. This study aimed to investigate the potential use of Tamarix articulata, quercetin and epigallocatechin gallate (EGCG) in HCC and how these phytochemicals could epigenetically modulate the IGF axis using their impact on miR-1275...
August 18, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28817601/bortezomib-initiates-endoplasmic-reticulum-stress-elicits-autophagy-and-death-in-echinococcus-granulosus-larval-stage
#8
María Celeste Nicolao, Julia A Loos, Christian Rodriguez Rodrigues, Viviana Beas, Andrea C Cumino
Cystic echinococcosis (CE) is a worldwide distributed helminthic zoonosis caused by Echinococcus granulosus. Benzimidazole derivatives are currently the only drugs for chemotherapeutic treatment of CE. However, their low efficacy and the adverse effects encourage the search for new therapeutic targets. We evaluated the in vitro efficacy of Bortezomib (Bz), a proteasome inhibitor, in the larval stage of the parasite. After 96 h, Bz showed potent deleterious effects at a concentration of 5 μM and 0.5 μM in protoscoleces and metacestodes, respectively (P < 0...
2017: PloS One
https://www.readbyqxmd.com/read/28817488/risk-management-of-hospitalized-psychiatric-patients-taking-multiple-qtc-prolonging-drugs
#9
Eline Vandael, Bert Vandenberk, Rik Willems, Johan Reyntens, Joris Vandenberghe, Veerle Foulon
PURPOSE/BACKGROUND: Drug-related QTc prolongation has been linked with Torsade de Pointes and sudden cardiac death. The objective of this study was to investigate the impact of starting an additional QTc-prolonging drug on the QTc interval of psychiatric inpatients. METHODS: An observational study was performed between May 2011 and December 2014 in 6 Belgian psychiatric hospitals. Inpatients who were already taking 1 QTc-prolonging drug or more could be included in the study when an additional QTc-prolonging drug was started...
August 16, 2017: Journal of Clinical Psychopharmacology
https://www.readbyqxmd.com/read/28816544/animal-inflammation-based-models-of-depression-and-their-application-to-drug-discovery
#10
Li Ma, Konstantin A Demin, Tatyana O Kolesnikova, Sergey L Kharsko, Xiaokang Zhu, Xiaodong Yuan, Cai Song, Darya A Meshalkina, Brian E Leonard, Li Tian, Allan V Kalueff
Depression, anxiety and other affective disorders are globally widespread and severely debilitating human brain diseases. Despite their high prevalence and mental health impact, affective pathogenesis is poorly understood, and often remains recurrent and resistant to treatment. The lack of efficient antidepressants and presently limited conceptual innovation necessitate novel approaches and new drug targets in the field of antidepressant therapy. Areas covered: Herein, the authors discuss the emerging role of neuro-immune interactions in affective pathogenesis, which can become useful targets for CNS drug discovery, including modulating neuroinflammatory pathways to alleviate affective pathogenesis...
August 17, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28816066/stressing-the-epi-genome-dealing-with-ros-in-cancer
#11
Akshay V Bhat, Shainan Hora, Ananya Pal, Sudhakar Jha, Reshma Taneja
SIGNIFICANCE: Growing evidence indicates cross-talk between Reactive oxygen species (ROS) and several key epigenetic processes like DNA methylation, histone modifications and miRNAs in normal physiology and human pathologies including cancer. This review focuses on how ROS-induced oxidative stress, metabolic intermediates and epigenetic processes influence each other in various cancers. Recent Advances: ROS alters chromatin structure and metabolism which impact the epigenetic landscape in cancer cells...
August 17, 2017: Antioxidants & Redox Signaling
https://www.readbyqxmd.com/read/28815420/road-map-for-the-structure-based-design-of-selective-covalent-hcv-ns3-4a-protease-inhibitors
#12
REVIEW
Letitia Shunmugam, Pritika Ramharack, Mahmoud E S Soliman
Over the last 2 decades, covalent inhibitors have gained much popularity and is living up to its reputation as a powerful tool in drug discovery. Covalent inhibitors possess many significant advantages including increased biochemical efficiency, prolonged duration and the ability to target shallow, solvent exposed substrate-binding domains. However, rapidly mounting concerns over the potential toxicity, highly reactive nature and general lack of selectivity have negatively impacted covalent inhibitor development...
August 16, 2017: Protein Journal
https://www.readbyqxmd.com/read/28814468/persistent-effects-of-acute-stress-on-fear-and-drug-seeking-in-a-novel-model-of-the-comorbidity-between-post-traumatic-stress-disorder-and-addiction
#13
Christie L Pizzimenti, Tom M Navis, K Matthew Lattal
Even following long periods of abstinence, individuals with anxiety disorders have high rates of relapse to drugs of abuse. Although many current models of relapse demonstrate effects of acute stress on drug-seeking, most of these studies examine stressful experiences that occur in close temporal and physical proximity to the reinstatement test. Here, we assess the effects of a stressful experience in one context on fear and drug-seeking in a different context. We adapt the stress-enhanced fear learning procedure to examine impacts on drug-seeking long after the stressful experience occurred...
September 2017: Learning & Memory
https://www.readbyqxmd.com/read/28814310/modelling-the-benefits-of-long-acting-or-transmission-blocking-drugs-for-reducing-plasmodium-falciparum-transmission-by-case-management-or-by-mass-treatment
#14
Michael T Bretscher, Jamie T Griffin, Azra C Ghani, Lucy C Okell
BACKGROUND: Anti-malarial drugs are an important tool for malaria control and elimination. Alongside their direct benefit in the treatment of disease, drug use has a community-level effect, clearing the reservoir of infection and reducing onward transmission of the parasite. Different compounds potentially have different impacts on transmission-with some providing periods of prolonged chemoprophylaxis whilst others have greater transmission-blocking potential. The aim was to quantify the relative benefit of such properties for transmission reduction to inform target product profiles in the drug development process and choice of first-line anti-malarial treatment in different endemic settings...
August 16, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28812389/evolocumab-for-the-treatment-of-hypercholesterolemia
#15
Brian Tomlinson, Miao Hu, Yuzhen Zhang, Paul Chan, Zhong-Min Liu
Evolocumab is a fully human monoclonal immunoglobulin G2 directed against human proprotein convertase subtilisin/kexin type 9 (PCSK9). It is administered by subcutaneous injection every 2 weeks or once monthly. Area covered: Herein, the authors discuss the rationale for inhibiting PCSK9 and describe the pharmacodynamics, pharmacokinetics and clinical trials with evolocumab. Evolocumab reduces low density lipoprotein cholesterol (LDL-C) levels by 50 to 60% in most patients with and without background treatment with statins or other lipid lowering agents...
August 16, 2017: Expert Opinion on Biological Therapy
https://www.readbyqxmd.com/read/28812207/the-vaginal-microbiome-and-its-potential-to-impact-efficacy-of-hiv-pre-exposure-prophylaxis-for-women
#16
REVIEW
Jennifer Velloza, Renee Heffron
PURPOSE OF REVIEW: This review describes existing evidence addressing the potential modulation of pre-exposure prophylaxis (PrEP) products, specifically 1% tenofovir (TFV) gel and oral tenofovir-based PrEP, by vaginal dysbiosis and discusses future considerations for delivering novel, long-acting PrEP products to women at high risk for vaginal dysbiosis and HIV. RECENT FINDINGS: We describe results from analyses investigating the modification of PrEP efficacy by vaginal dysbiosis and studies of biological mechanisms that could render PrEP ineffective in the presence of specific microbiota...
August 15, 2017: Current HIV/AIDS Reports
https://www.readbyqxmd.com/read/28811192/relative-reinforcing-effects-of-second-generation-synthetic-cathinones-acquisition-of-self-administration-and-fixed-ratio-dose-response-curves-in-rats
#17
REVIEW
Brenda M Gannon, Kayla I Galindo, Melson P Mesmin, Agnieszka Sulima, Kenner C Rice, Gregory T Collins
"Bath salts" preparations contain synthetic cathinones which interact with monoamine transporters and function as either monoamine uptake inhibitors or releasers. 3,4-Methylenedioxypyrovalerone (MDPV), 3,4-methylenedioxymethcathinone (methylone), and 4-methylmethcathinone (mephedrone) were three of the most common cathinones (i.e., "first-generation" cathinones); however, after the US Drug Enforcement Administration placed them under Schedule I regulations, they were replaced with structurally related cathinones that were not subject to regulations (i...
August 12, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28809994/the-static-physician-s-global-assessment-of-genitalia-a-clinical-outcome-measure-for-the-severity-of-genital-psoriasis
#18
Joseph F Merola, Alison Potts Bleakman, Alice B Gottlieb, Alan Menter, April N Naegeli, Robert Bissonnette, Lyn Guenther, John Sullivan, Kim Meeuwis, Kyoungah See, Kristina Callis Duffin
<p>Introduction: Genital psoriasis is a common but frequently overlooked manifestation of psoriasis with a considerable impact on patients' quality of life. Currently no validated clinical trial outcome measures exist to assess genital psoriasis severity that meet regulatory agency requirements.</p> <p>Methods: This study describes the development of the static Physician's Global Assessment of Genitalia (sPGA-G) scale, a clinical outcome measure for the assessment of genital psoriasis severity that accounts for the erythematous clinical presentation of genital psoriasis...
August 1, 2017: Journal of Drugs in Dermatology: JDD
https://www.readbyqxmd.com/read/28809993/adalimumab-in-chronic-plaque-psoriasis-a-clinical-guide
#19
Jashin J Wu, W C Valdecantos
<p>Psoriasis is a common, inflammatory disease that manifests itself as lesions on the skin, which greatly impacts the physical and psychological wellbeing of those affected. The current goal of treatment in psoriasis is to improve the signs and symptoms of disease, whilst minimizing the burden of disease on patient health-related quality of life. Psoriasis can also be associated with other comorbidities such as joint disease, cardiovascular disease, and depression, which can add to the complexity of treatment...
August 1, 2017: Journal of Drugs in Dermatology: JDD
https://www.readbyqxmd.com/read/28809437/the-conditional-stimulation-of-rat-organic-cation-transporter-2-but-not-its-human-ortholog-by-mesoridazine-the-possibility-of-the-involvement-of-the-high-affinity-binding-site-of-the-transporter-in-the-stimulation
#20
Sungwoo Hyung, Wonji Pyeon, Ji Eun Park, Yoo-Kyung Song, Suk-Jae Chung
OBJECTIVES: To study the functional consequences of the human and rat forms of OCT2 in the presence of phenothiazines. METHODS: MDCK cells expressing human or rat OCT2 were established, and MPP+ transport was determined by uptake assays. Concentration dependency was studied for the stimulatory/inhibitory effects of phenothiazines on MPP+ transport. KEY FINDINGS: Among the 11 phenothiazines examined, the majority were found to have comparable effects on transporter function between the orthologous forms, while three phenothiazines, particularly mesoridazine, had complex impacts on transporter function...
August 15, 2017: Journal of Pharmacy and Pharmacology
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