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https://www.readbyqxmd.com/read/28651259/new-biguanides-as-anti-diabetic-agents-part-i-synthesis-and-evaluation-of-1-substituted-biguanide-derivatives-as-anti-diabetic-agents-of-type-ii-diabetes-insulin-resistant
#1
Samir Y Abbas, Wahid M Basyouni, Khairy A M El-Bayouk, Wael M Tohamy, Hanan F Aly, Azza Arafa, Mahmoud S Soliman
New 1-substituted-biguanide hydrochloride salts were synthesized via reacting benzo[1,3-d]dioxol-5-amine, phenylhydrazine, N,N-dimethylhydrazinecarboxamide, benzohydrazide and 2-phenyl acetohydrazide with dicyandiamide in acidic medium. Structures of the obtained biguanide salts were characterized by spectroscopic tools. The synthesized compounds were screened for their anti-diabetic activity with standard metformin drug. Oral treatment of hyperglycemic rats with the synthesized biguanide derivatives significantly decreased the elevated blood glucose level...
June 26, 2017: Drug Research
https://www.readbyqxmd.com/read/28651173/development-validation-and-clinical-application-of-a-method-for-the-simultaneous-quantification-of-lamivudine-emtricitabine-and-tenofovir-in-dried-blood-and-dried-breast-milk-spots-using-lc-ms-ms
#2
Catriona Waitt, Sujan Diliiy Penchala, Adeniyi Olagunju, Alieu Amara, Laura Else, Mohammed Lamorde, Saye Khoo
OBJECTIVES: To present the validation and clinical application of a LC-MS/MS method for the quantification of lamivudine (3TC), emtricitabine (FTC) and tenofovir (TFV) in dried blood spots (DBS) and dried breast milk spots (DBMS). METHODS: DBS and DBMS were prepared from 50 and 30μL of drug-spiked whole blood and human breast milk, respectively. Following extraction with acetonitrile and water, chromatographic separation utilised a Synergi polar column with a gradient mobile phase program consisting of 0...
June 17, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28650949/efficacy-and-safety-of-tranexamic-acid-in-orthopedic-fracture-surgery-a-meta-analysis-and-systematic-literature-review
#3
Kamil Amer, Saqib Rehman, Christopher Haydel
BACKGROUND: Tranexamic acid (TXA) is an anti-fibrinolytic drug that has been shown to be effective in reducing blood loss and the need for transfusions after several orthopedic surgeries. However, the effectiveness of TXA use in orthopedic fracture surgeries still remains unclear. The purpose of this meta-analysis was to review existing literature with interest in the effectiveness and safety of TXA treatment in reducing total blood loss and transfusion rates for patients who underwent surgery for fracture repairs...
June 12, 2017: Journal of Orthopaedic Trauma
https://www.readbyqxmd.com/read/28650917/long-term-changes-in-left-ventricular-mass-echocardiographic-findings-from-a-general-population
#4
Cesare Cuspidi, Fosca Quarti, Raffaella Dell'Oro, Rita Facchetti, Michele Bombelli, Carla Sala, Marijana Tadic, Guido Grassi, Giuseppe Mancia
AIM: We sought to assess the long-term changes in left ventricular (LV) mass in a population-based sample, focusing on new onset, persistence, regression and severity of LV hypertrophy (LVH), as well as on the demographic and clinical variables independently related to this dynamic process. METHODS: A total of 1113 participants with measurable echocardiographic parameters at baseline and after a 10-year follow-up were included in the analysis. Cut points for LVH were derived from current echocardiographic guidelines...
June 24, 2017: Journal of Hypertension
https://www.readbyqxmd.com/read/28650902/itpa-activity-in-adults-and-children-treated-with-or-without-azathioprine-relationship-between-tpmt-activity-thiopurine-metabolites-and-co-medications
#5
Boulieu Roselyne, Antony Citterio-Quentin, Mustapha Moulsma, Marie-Paule Gustin
BACKGROUND: The implication of inosine triphosphate pyrophosphatase (ITPA) on thiopurine drug response variability has been investigated but little data is available on its role on thiopurine metabolites. ITPA' ability to modify the thiopurine metabolite levels currently used to optimize azathioprine (AZA) therapy in relation to TPMT activity, the aim of this study is to investigate ITPA phenotype in a large population and to evaluate the relation between ITPA and TPMT activities and thiopurine metabolites...
June 22, 2017: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/28650422/the-effects-of-valsartan-on-renal-klotho-expression-and-oxidative-stress-in-alleviation-of-cyclosporine-nephrotoxicity
#6
Sina Raeisi, Amir Ghorbanihaghjo, Hassan Argani, Siavoush Dastmalchi, Babollah Ghasemi, Teimour Ghazizadeh, Nadereh Rashtchizadeh, Mahboob Nemati, Mehran Mesgari Abbasi, Nasrin Bargahi, Hossein Samadi Kafil, Amir Mansour Vatankhah
BACKGROUND: Nephrotoxicity side effect of the immunosuppressive drug, cyclosporine A (CsA), can be a major issue in transplantation medicine. Cyclosporine A-induced nephrotoxicity is multifactorial but oxidative stress has a critical role in this process. It has been demonstrated that Valsartan (Val) as an angiotensin receptor blocker has renoprotective effects, but the molecular mechanisms responsible for the renal protection, independent from its blood pressure lowering effect, have not yet been fully understood...
June 23, 2017: Transplantation
https://www.readbyqxmd.com/read/28649132/reassessment-of-subacute-mptp-treated-mice-as-animal-model-of-parkinson-s-disease
#7
Qiu-Shuang Zhang, Yang Heng, Zheng Mou, Ju-Yang Huang, Yu-He Yuan, Nai-Hong Chen
1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) mouse model remains the most commonly used animal model of Parkinson's disease (PD). There are three MPTP-treatment schemes: acute, subacute and chronic. Considering the advantages of the period and similarity to PD, the subacute model was often chosen to assess the validity of new candidates, but the changes caused by the subacute MPTP treatment and the appropriate positive control for this model remain to be further confirmed. The aim of this study was: 1 to estimate the value of the subacute MPTP mouse model in aspects of behavioral performance, biochemical changes and pathological abnormalities, and 2 to find effective positive drugs...
June 26, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28649076/renal-clearance-and-urinary-excretion-of-omeprazole-in-healthy-female-volunteers-in-pakistan
#8
Nazia Qadir, Tanweer Khaliq, Rai Altaf Hussain, Ghulam Abbas Shah, Sadia Asharaf, Ahmad Raza, Nadia Noor
Omeprazole is a widely prescribed proton pump inhibitor to treat various gastric acid hyper secretion disorders. The present study was designed to evaluate the renal clearance and urinary excretion of omeprazole in eight healthy female volunteers to increase the understanding of the contributing factors such as demographics variability in the renal clearance and urinary excretion of omeprazole under indigenous conditions. The urine and blood samples were collected 0.5, 1, 1.5, 2, 3, 4, 6, 8 hours after oral administration of enteric coated omeprazole (20 mg) and drug concentration in the samples was determined by High Performance Liquid Chromatography (HPLC) with C18 column and UV detector...
March 2017: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28648978/the-thymus-and-activation-regulated-chemokine-tarc-level-in-serum-at-an-early-stage-of-a-drug-eruption-is-a-prognostic-biomarker-of-severity-of-systemic-inflammation
#9
Takayoshi Komatsu-Fujii, Yuko Chinuki, Hiroyuki Niihara, Kenji Hayashida, Masataka Ohta, Ryota Okazaki, Sakae Kaneko, Eishin Morita
BACKGROUND: In severe drug eruptions, precise evaluation of disease severity at an early stage is needed to start appropriate treatment. It is not always easy to diagnose these conditions at their early stage. In addition, there are no reported prognostic biomarkers of disease severity in drug eruptions. The aim of this study was to test whether the thymus and activation-regulated chemokine (TARC) level in serum at an early stage of a drug eruption can serve as a prognostic biomarker of systemic inflammation...
June 22, 2017: Allergology International: Official Journal of the Japanese Society of Allergology
https://www.readbyqxmd.com/read/28648975/effect-of-extract-of-pueraria-tuberosa-on-expression-of-hypoxia-inducible-factor-1%C3%AE-and-vascular-endothelial-growth-factor-in-kidney-of-diabetic-rats
#10
Rashmi Shukla, Nidhi Pandey, Somanshu Banerjee, Yamini B Tripathi
BACKGROUNDS: Kidney hypoxia represents a unifying mechanism in the pathogenesis of diabetic nephropathy. Hypoxia-induced factor (HIF)-1α mediates the metabolic responses of renal hypoxia by modulating the expression of VEGF. In the present study, we investigated the effect of Pueraria tuberosa extract (PTY-2r) on the expression of HIF-1α, VEGF and nephrin in streptozotocin (STZ) induced diabetic nephropathy (DN). METHODS: The model of diabetic nephropathy (DN) was produced by intraperitoneal injection of 55mg/kg of STZ and maintained for 60days...
June 22, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28648928/pg2-a-botanically-derived-drug-extracted-from-astragalus-membranaceus-promotes-proliferation-and-immunosuppression-of-umbilical-cord-derived-mesenchymal-stem-cells
#11
Yu-Hua Chao, Kang-Hsi Wu, Chiao-Wen Lin, Shun-Fa Yang, Wan-Ru Chao, Ching-Tien Peng, Han-Ping Wu
ETHNOPHARMACOLOGICAL RELEVANCE: Astragalus membranaceus is used to manage the deficiency of vital energy in traditional Chinese medicine and confirmed to have many biological functions. Mesenchymal stem cells (MSCs) possess immunosuppressive effects, and are widely used for regenerative medicine and immune disorders. AIMS OF STUDY: This study investigated the effects of Astragalus polysaccharides (APS) on umbilical cord-derived MSCs (UCMSCs), including morphology, surface marker expression, proliferation, differentiation, and in-vitro and in-vivo immunosuppressive capacities...
June 22, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28646805/natural-cancer-therapy-and-prevention-targeted-on-cancer-cells-and-cancer-stem-cells-based-on-the-cytochrome-p45o-enzyme-cyp1b1-a-commentary
#12
William R Ware
The importance of the P450 enzyme CYP1B1 in both cancer therapy and prevention are reviewed and evidence is discussed, which provides strong biological plausibility for the therapeutic merits of this approach. The significant resistance to chemotherapy among common cancers, and the realization that in many cases chemotherapy leaves behind drug-resistant cancer cells that eventually cause recurrence and metastatic disease, has recently prompted the search for natural compounds that would circumvent this problem...
June 23, 2017: Alternative Therapies in Health and Medicine
https://www.readbyqxmd.com/read/28646491/sickle-cells-produce-functional-immune-modulators-and-cytotoxics
#13
Chiao-Wang Sun, Li-Chen Wu, Peter L Knopick, David S Bradley, Tim Townes, David S Terman
Sickle erythrocytes' (SSRBCs) unique physical adaptation to hypoxic conditions renders them able to home to hypoxic tumor niches in vivo, shut down tumor blood flow and induce tumoricidal responses. SSRBCs are also useful vehicles for transport of encapsulated drugs and oncolytic virus into hypoxic tumors with enhanced anti-tumor effects. In search of additional modes for arming sickle cells with cytotoxics, we turned to a lentiviral β-globin vector with optimized Locus Control Region/β-globin coding region/promoter/enhancers...
June 24, 2017: American Journal of Hematology
https://www.readbyqxmd.com/read/28646338/chemotherapy-induced-gastrointestinal-toxicity-is-associated-with-changes-in-serum-and-urine-metabolome-and-fecal-microbiota-in-male-sprague-dawley-rats
#14
Richard A Forsgård, Vannina G Marrachelli, Katri Korpela, Rafael Frias, Maria Carmen Collado, Riitta Korpela, Daniel Monleon, Thomas Spillmann, Pia Österlund
PURPOSE: Chemotherapy-induced gastrointestinal toxicity (CIGT) is a complex process that involves multiple pathophysiological mechanisms. We have previously shown that commonly used chemotherapeutics 5-fluorouracil, oxaliplatin, and irinotecan damage the intestinal mucosa and increase intestinal permeability to iohexol. We hypothesized that CIGT is associated with alterations in fecal microbiota and metabolome. Our aim was to characterize these changes and examine how they relate to the severity of CIGT...
June 23, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28645518/blood-gas-analyzer-accuracy-of-glucose-measurements
#15
Yafen Liang, Jonathan Wanderer, James H Nichols, David Klonoff, Mark J Rice
OBJECTIVE: To investigate the comparability of glucose levels measured with blood gas analyzers (BGAs) and by central laboratories (CLs). MATERIAL AND METHODS: Glucose measurements obtained between June 1, 2007, and March 1, 2016, at the Vanderbilt University Medical Center were reviewed. The agreement between CL and BGA results were assessed using Bland-Altman, consensus error grid (CEG), and surveillance error grid (SEG) analyses. We further analyzed the BGAs' performance against the US Food and Drug Administration (FDA) 2014 draft guidance and 2016 final guidance for blood glucose monitoring and the International Organization for Standardization (ISO) 15197:2013 standard...
June 7, 2017: Mayo Clinic Proceedings
https://www.readbyqxmd.com/read/28645468/aldhs-in-normal-and-malignant-hematopoietic-cells-potential-new-avenues-for-treatment-of-aml-and-other-blood-cancers
#16
Maura Gasparetto, Clayton A Smith
Multiple studies have demonstrated that ALDH1A1 is elevated in hematopoietic stem cells (HSCs). As a means to better characterize such cells, we previously developed the fluorescent ALDH1A1 substrate Aldefluor to facilitate HSC identification and isolation. This has proven useful for counting and isolating HSCs from human bone marrow, peripheral blood and cord blood as well as stem cells in other tissues and organisms. Given the high level expression of ALDH1A1, we explored its biology and that of other ALDHs in HSCs and found that ALDH1A1 and ALDH3A1 were important in metabolizing reactive aldehydes (RAlds) and reactive oxygen species (ROS)...
June 20, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28644562/efficacy-of-ipragliflozin-as-monotherapy-or-as-add-on-therapy-with-other-oral-antidiabetic-medications-in-treating-type-2-diabetes-in-japanese-patients-with-inadequate-glycemic-control-a-subgroup-analysis-based-on-patient-characteristics
#17
Takeshi Osonoi, Shinya Nakamoto, Miyoko Saito, Atsuko Tamasawa, Hidenori Ishida, Yusuke Osonoi
AIMS/INTRODUCTION: The aim of the present study was to evaluate the efficacy and safety of ipragliflozin in treating Japanese type 2 diabetic patients with inadequate glycemic control by investigating diurnal variations of blood glucose and body composition. MATERIALS AND METHODS: This was an investigator-initiated, multicenter, prospective study with a 6-month treatment period. The primary outcome investigated was change in hemoglobin A1c levels from baseline. Secondary outcomes included changes in fasting plasma glucose, insulin resistance, variations in 24-h glucose levels detected by continuous glucose monitoring, body weight, body composition, waist circumference, and serum lipids...
June 23, 2017: Journal of Diabetes Investigation
https://www.readbyqxmd.com/read/28644038/critical-review-on-the-analytical-techniques-for-the-determination-of-the-oldest-statin-atorvastatin-in-bulk-pharmaceutical-formulations-and-biological-fluids
#18
K S Kokilambigai, R Seetharaman, K S Lakshmi
Statins are a group of medicines that can help to lower the level of low-density-lipoprotein(LDL) cholesterol "bad cholesterol" in the blood. Having a high level of LDL cholesterol is potentially dangerous, as it can lead to a hardening and narrowing of arteries (atherosclerosis) and cardiovascular disease (CVD), Atorvastatin is one of the oldest member of the statin family and is used in the treatment of dyslipidemia and the prevention of cardiovascular disease. Atorvastatin was first made in August 1985 and from 1996 to 2012 under the trade name Lipitor, atorvastatin became the world's best selling drug...
June 23, 2017: Critical Reviews in Analytical Chemistry
https://www.readbyqxmd.com/read/28641720/fenofibrate-attenuates-hypertension-in-goldblatt-hypertensive-rats-role-of-20-hydroxyeicosatetraenoic-acid-in-the-nonclipped-kidney
#19
Alexandra Sporková, Věra Čertíková Chábová, Šárka Doleželová, Šárka Jíchová, Libor Kopkan, Zdeňka Vaňourková, Elzbieta Kompanowska-Jezierska, Janusz Sadowski, Hana Maxová, Luděk Červenka
BACKGROUND: There is vast evidence that the renin-angiotensin system is not the sole determinant of blood pressure (BP) elevation in human renovascular hypertension or the relevant experimental models. This study tested the hypothesis that kidney deficiency of 20-hydroxyeicosatetraenoic acid (20-HETE), a product of cytochrome P450 (CYP)-dependent ω-hydroxylase pathway of arachidonic acid metabolism, is important in the pathophysiology of the maintenance phase of 2-kidney, 1-clip (2K1C) Goldblatt hypertension...
June 2017: American Journal of the Medical Sciences
https://www.readbyqxmd.com/read/28641707/analysis-of-transmitted-hiv-drug-resistance-from-2005-to-2015-in-victoria-australia-a-comparison-of-the-old-and-the-new
#20
Jodie D'Costa, Megan Gooey, Nicole Richards, Rizmina Sameer, Elaine Lee, Doris Chibo
Background: Baseline genotyping is part of standard-of-care treatment. It reveals that transmitted drug resistance (TDR) continues to be important for the management of HIV infection. Attention is typically focused on determining whether resistance to the protease inhibitors (PI) and reverse transcriptase inhibitors (RTI) occurs. However, the increasing use of integrase inhibitors (INIs) raises a concern that TDR to this class of antiretroviral drug may also occur. Methods: PI and RTI drug resistance genotyping was performed on blood samples collected between 2005 and 2015 from 772 treatment-naïve Victorian patients infected with HIV within the previous 12 months...
June 23, 2017: Sexual Health
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