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https://www.readbyqxmd.com/read/29333040/pharmacological-screening-of-trachyspermum-ammi-for-antihyperlipidemic-activity-in-triton-x-100-induced-hyperlipidemia-rat-model
#1
Uzma Saleem, Saba Riaz, Bashir Ahmad, Mohammad Saleem
Background: Mortality rate is increasing due to cardiovascular problems throughout the world. These cardiac problems are directly associated with dyslipidemia. Aim: The aim of this study was to evaluate the antihyperlipidemic effect of aqueous extract and methanol extract of Trachyspermum ammi at 1 g/kg, 3 g/kg, and 5 g/kg dose levels in rats. Materials and Methods: For this purpose, 45 male albino rats were used and randomly divided into nine equal groups (n = 5)...
December 2017: Pharmacognosy Research
https://www.readbyqxmd.com/read/29297315/utilizing-random-forest-qsar-models-with-optimized-parameters-for-target-identification-and-its-application-to-target-fishing-server
#2
Kyoungyeul Lee, Minho Lee, Dongsup Kim
BACKGROUND: The identification of target molecules is important for understanding the mechanism of "target deconvolution" in phenotypic screening and "polypharmacology" of drugs. Because conventional methods of identifying targets require time and cost, in-silico target identification has been considered an alternative solution. One of the well-known in-silico methods of identifying targets involves structure activity relationships (SARs). SARs have advantages such as low computational cost and high feasibility; however, the data dependency in the SAR approach causes imbalance of active data and ambiguity of inactive data throughout targets...
December 28, 2017: BMC Bioinformatics
https://www.readbyqxmd.com/read/29289377/treatment-of-paraphilic-disorders-in-sexual-offenders-or-men-with-a-risk-of-sexual-offending-with-luteinizing-hormone-releasing-hormone-agonists-an-updated-systematic-review
#3
REVIEW
Daniel Turner, Peer Briken
BACKGROUND: Different pharmacologic agents are used in the treatment of paraphilic disorders in sexual offenders or men with a risk of sexual offending, with luteinizing hormone-releasing hormone (LHRH) agonists being the agents introduced more recently to treatment regimens. AIM: To summarize the relevant literature concerning LHRH agonist treatment of paraphilic disorders in sexual offenders and update the previously published systematic review by Briken et al (J Clin Psychiatry 2003;64:890-897)...
January 2018: Journal of Sexual Medicine
https://www.readbyqxmd.com/read/29249913/new-strategies-to-improve-polypectomy-during-colonoscopy
#4
Michael B Wallace
In the United States, colorectal cancer (CRC) is the second-leading cause of cancer-related deaths. The most effective strategy for prevention of CRC is to screen for and remove precancerous polyps. There are various ways to screen for CRC. In the United States, the most common method is colonoscopy. Polyps are classified primarily through pathology. Size is the primary risk factor for malignancy. In general, the bigger the polyp, the greater the risk for malignancy. There are 3 basic options for removal: standard polypectomy; advanced resection techniques, known as endoscopic mucosal resection (EMR) and endoscopic submucosal dissection (ESD); and surgical removal...
October 2017: Gastroenterology & Hepatology
https://www.readbyqxmd.com/read/29227878/harm-reduction-based-and-peer-supported-hepatitis-c-treatment-for-people-who-inject-drugs-in-georgia
#5
Tamar Kikvidze, Niklas Luhmann, Elisabeth Avril, Maia Butsashvili, Konstantine Labartkava, Aurélie Etienne, Diane Le Pluart, Ina Inaridze, Ana Gamezardashvili, David Kharshiladze, Julie Bouscaillou
BACKGROUNDS: Georgia faces high HCV rates (5.4% of chronic cases in general population) with an epidemic concentrated among people who inject drugs (PWID). A National HCV Elimination Program (NHCEP), was launched in April 2015, aiming to eliminate HCV by 2020. To succeed, this program must develop tailored interventions to enroll PWID in treatment. INTERVENTION: We implemented a pilot intervention to facilitate access to and retention of PWID in the NHCEP, and to prevent reinfection after treatment...
December 8, 2017: International Journal on Drug Policy
https://www.readbyqxmd.com/read/29215913/high-content-screening-comparison-of-cancer-drug-accumulation-and-distribution-in-two-dimensional-and-three-dimensional-culture-models-of-head-and-neck-cancer
#6
Feng Shan, David A Close, Daniel P Camarco, Paul A Johnston
High cancer drug development attrition rates have provoked considerable debate about whether the two-dimensional tumor growth inhibition high-throughput screening assays used in pre-clinical lead discovery adequately reflect solid tumor complexity. We used automated high-content screening image acquisition and analysis methods to compare fluorescent drug uptake, accumulation, and distribution in Cal33 and FaDu head and neck cancer (HNC) monolayer and multicellular tumor spheroid (MCTS) models. Ellipticine, idarubicin, daunorubicin, and doxorubicin were studied because of their fluorescent properties and broad anti-tumor activities...
December 7, 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29201009/in-vitro-and-in-silico-risk-assessment-in-acquired-long-qt-syndrome-the-devil-is-in-the-details
#7
REVIEW
William Lee, Monique J Windley, Jamie I Vandenberg, Adam P Hill
Acquired long QT syndrome, mostly as a result of drug block of the Kv11. 1 potassium channel in the heart, is characterized by delayed cardiac myocyte repolarization, prolongation of the T interval on the ECG, syncope and sudden cardiac death due to the polymorphic ventricular arrhythmia Torsade de Pointes (TdP). In recent years, efforts are underway through the Comprehensive in vitro proarrhythmic assay (CiPA) initiative, to develop better tests for this drug induced arrhythmia based in part on in silico simulations of pharmacological disruption of repolarization...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/29044549/effects-of-clioquinol-on-the-scuticociliatosis-causing-protozoan-miamiensis-avidus-in-olive-flounder-paralichthys-olivaceus
#8
J-H Lee, J-J Park, J-H Choi, S-Y Kang, Y-J Kang, K H Park
Scuticociliatosis is a devastating and intractable protozoal disease in olive flounder, leading to a significant loss throughout the year. This study aimed to investigate a systemically effective antiscuticociliatosis agent for olive flounder for better absorption into the infected internal organs. The in vitro and in vivo antiscuticociliatosis effects of clioquinol (CQ) were examined after screening 30 biocidal agents against the highly pathogenic scuticociliate Miamiensis avidus. CQ was the most potent in vitro drug of those tested against cultured M...
October 17, 2017: Journal of Fish Diseases
https://www.readbyqxmd.com/read/28979759/mass-spectrometric-directed-system-for-the-continuous-flow-synthesis-and-purification-of-diphenhydramine
#9
Bradley P Loren, Michael Wleklinski, Andy Koswara, Kathryn Yammine, Yanyang Hu, Zoltan K Nagy, David H Thompson, R Graham Cooks
A highly integrated approach to the development of a process for the continuous synthesis and purification of diphenhydramine is reported. Mass spectrometry (MS) is utilized throughout the system for on-line reaction monitoring, off-line yield quantitation, and as a reaction screening module that exploits reaction acceleration in charged microdroplets for high throughput route screening. This effort has enabled the discovery and optimization of multiple routes to diphenhydramine in glass microreactors using MS as a process analytical tool (PAT)...
June 1, 2017: Chemical Science
https://www.readbyqxmd.com/read/28951824/intraocular-in%C3%A2-vivo-imaging-of-pancreatic-islet-cell-physiology-pathology
#10
REVIEW
Ingo B Leibiger, Per-Olof Berggren
BACKGROUND: Diabetes mellitus has reached epidemic proportions and requires new strategies for treatment. Unfortunately, the efficacy of treatment regimens on maintaining/re-gaining functional beta cell mass can, at the present, only be determined indirectly. Direct monitoring of beta cell mass is complicated by the anatomy of the endocrine pancreas, which consists of thousands to a million of discrete micro-organs, i.e. islets of Langerhans, which are scattered throughout the pancreas...
September 2017: Molecular Metabolism
https://www.readbyqxmd.com/read/28889384/spheroid-cultures-of-primary-urothelial-cancer-cells-cancer-tissue-originated-spheroid-ctos-method
#11
Takahiro Yoshida, Hiroaki Okuyama, Hiroko Endo, Masahiro Inoue
Increasingly, it has been recognized that studying cancer samples from individual patients is important for the development of effective therapeutic strategies and in endeavors to overcome therapy resistance. Primary cultures of cancer cells acutely dissected from individual patients can provide a platform that enables the study and characterization of individual tumors. To that end, we have developed a method for preparing cancer cells in the form of multi-cellular spheroids. The cells can be derived from patient tumors (primary cells), from patient-derived xenografts, or from genetically- or chemically induced animal tumors...
2018: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28835636/potential-inhibitors-designed-against-ndm-1-type-metallo-%C3%AE-lactamases-an-attempt-to-enhance-efficacies-of-antibiotics-against-multi-drug-resistant-bacteria
#12
Asad U Khan, Abid Ali, Danishuddin, Gaurava Srivastava, Ashok Sharma
NDM-1 and its variants are the most prevalent types of metallo-β-lactamases, hydrolyze almost all antibiotics of β-lactam group leading to multiple-drug resistance in bacteria. No inhibitor has yet been obtained for NDM-1 or other class of metallo-β-lactamases. Therefore, strategies to identify novel anti-β-lactamase agents with specific mechanisms of action are the need of an hour. In this study, we have reported the discovery of novel non-β-lactam inhibitors against NDM-1 by multi-step virtual screening approach...
August 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28685162/in-vivo-indicators-of-cytoplasmic-vacuolar-and-extracellular-ph-using-phluorin2-in-candida-albicans
#13
Hélène Tournu, Arturo Luna-Tapia, Brian M Peters, Glen E Palmer
Environmental or chemically induced stresses often trigger physiological responses that regulate intracellular pH. As such, the capacity to detect pH changes in real time and within live cells is of fundamental importance to essentially all aspects of biology. In this respect, pHluorin, a pH-sensitive variant of green fluorescent protein, has provided an invaluable tool to detect such responses. Here, we report the adaptation of pHluorin2 (PHL2), a substantially brighter variant of pHluorin, for use with the human fungal pathogen Candida albicans...
July 2017: MSphere
https://www.readbyqxmd.com/read/28669605/industrial-medicinal-chemistry-insights-neuroscience-hit-generation-at-janssen
#14
REVIEW
Gary Tresadern, Frederik J R Rombouts, Daniel Oehlrich, Gregor Macdonald, Andres A Trabanco
The role of medicinal chemistry has changed over the past 10 years. Chemistry had become one step in a process; funneling the output of high-throughput screening (HTS) on to the next stage. The goal to identify the ideal clinical compound remains, but the means to achieve this have changed. Modern medicinal chemistry is responsible for integrating innovation throughout early drug discovery, including new screening paradigms, computational approaches, novel synthetic chemistry, gene-family screening, investigating routes of delivery, and so on...
June 29, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28590392/pilot-studies-examining-feasibility-of-substance-use-disorder-screening-and-treatment-linkage-at-urban-sexually-transmitted-disease-clinics
#15
Jan Gryczynski, Courtney D Nordeck, Shannon Gwin Mitchell, Kathleen R Page, Luke L Johnsen, Kevin E O'Grady, Robert P Schwartz
BACKGROUND: Sexually transmitted disease (STD) clinics provide critical public health services for screening and treatment of sexually transmitted infections throughout the United States. These settings serve high-risk populations, often on a walk-in basis, and may be promising venues for integrating substance use disorder (SUD) services. METHODS: We report findings from 2 pilot studies conducted at Baltimore City Health Department's STD clinics. The screening study characterized rates of SUDs among STD clinic patients...
September 2017: Journal of Addiction Medicine
https://www.readbyqxmd.com/read/28573153/optical-imaging-of-the-rat-brain-suggests-a-previously-missing-link-between-top-down-and-bottom-up-nervous-system-function
#16
Susan A Greenfield, Antoine-Scott Badin, Giovanni Ferrati, Ian M Devonshire
Optical imaging with voltage-sensitive dyes enables the visualization of extensive yet highly transient coalitions of neurons (assemblies) operating throughout the brain on a subsecond time scale. We suggest that operating at the mesoscale level of brain organization, neuronal assemblies may provide a functional link between "bottom-up" cellular mechanisms and "top-down" cognitive ones within anatomically defined regions. We demonstrate in ex vivo rat brain slices how varying spatiotemporal dynamics of assemblies reveal differences not previously appreciated between: different stages of development in cortical versus subcortical brain areas, different sensory modalities (hearing versus vision), different classes of psychoactive drugs (anesthetics versus analgesics), different effects of anesthesia linked to hyperbaric conditions and, in vivo, depths of anesthesia...
July 2017: Neurophotonics
https://www.readbyqxmd.com/read/28566227/boosted-protease-inhibitor-monotherapy-versus-boosted-protease-inhibitor-plus-lamivudine-dual-therapy-as-second-line-maintenance-treatment-for-hiv-1-infected-patients-in-sub-saharan-africa-anrs12-286-mobidip-a-multicentre-randomised-parallel-open-label-superiority
#17
Laura Ciaffi, Sinata Koulla-Shiro, Adrien Bruno Sawadogo, Cheik Tidiane Ndour, Sabrina Eymard-Duvernay, Pretty Rosereine Mbouyap, Liliane Ayangma, Jacques Zoungrana, Ndeye Fatou Ngom Gueye, Mohamadou Diallo, Suzanne Izard, Guillaume Bado, Coumba Toure Kane, Avelin Fobang Aghokeng, Martine Peeters, Pierre Marie Girard, Vincent Le Moing, Jacques Reynes, Eric Delaporte
BACKGROUND: Despite satisfactory efficacy of WHO-recommended second-line antiretroviral treatment for patients with HIV in low-income countries, the need for simplified, low-cost, and less-toxic maintenance strategies remains high. We compared boosted protease inhibitor monotherapy with dual therapy with boosted protease inhibitor plus lamivudine in patients on second-line antiretrovial therapy (ART). METHODS: We did a multicentre, randomised, parallel, open-label, superiority, trial in the HIV services of five hospitals in sub-Saharan Africa (Yaoundé, Cameroon; Dakar, Senegal; and Bobo Dioulasso, Burkina Faso)...
September 2017: Lancet HIV
https://www.readbyqxmd.com/read/28545327/designing-of-inhibitors-against-ctx-m-15-type-%C3%AE-lactamase-potential-drug-candidate-against-%C3%AE-lactamases-producing-multi-drug-resistant-bacteria
#18
Abid Ali, Danishuddin, Lubna Maryam, Gaurava Srivastava, Ashok Sharma, Asad U Khan
CTX-M-15 are the most prevalent types of β-lactamases that hydrolyze almost all antibiotics of β-lactam group lead to multiple-antibiotic resistance in bacteria. Three β-lactam inhibitors are available for use in combination with different antibiotics of cephalosporine group against the CTX-M-15-producing strains. Therefore, strategies to identify novel anti β-lactamase agents with specific mechanisms of action are the need of an hour. In this study, we screened three novel non-β-lactam inhibitors against CTX-M-15 by multi-step virtual screening approach...
June 8, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28515725/application-of-zebrafish-models-in-inflammatory-bowel-disease
#19
REVIEW
Li Hanyang, Liu Xuanzhe, Chen Xuyang, Qiu Yujia, Fu Jiarong, Shen Jun, Ran Zhihua
Inflammatory bowel disease (IBD) is a chronic, recurrent, and remitting inflammatory disease with unclear etiology. As a clinically frequent disease, it can affect individuals throughout their lives, with multiple complications. Unfortunately, traditional murine models are not efficient for the further study of IBD. Thus, effective and convenient animal models are needed. Zebrafish have been used as model organisms to investigate IBD because of their suggested highly genetic similarity to humans and their superiority as laboratory models...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/28514994/active-syphilis-and-its-association-with-hiv-and-sexual-risk-behaviours-in-a-multicity-sample-of-men-who-have-sex-with-men-and-transgender-women-in-peru
#20
Lia N Pizzicato, Panagiotis Vagenas, Pedro Gonzales, Javier R Lama, Monica Pun, Jorge Sanchez, Frederick L Altice
Background: Syphilis in Peru is heavily concentrated in men who have sex with men (MSM) and transgender women (TGW). The aim of the present study was to understand the risk factors for active syphilis infection among MSM and TGW in Peru. Methods: Independent correlates suggestive of active syphilis infection were examined to better understand risk factors for syphilis in MSM and TGW, with separate analyses conducted based on location and among TGW. In 2011, 5101 MSM and TGW completed both self-report surveys and HIV and syphilis testing in five Peruvian cities...
May 18, 2017: Sexual Health
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