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https://www.readbyqxmd.com/read/28425040/schiff-base-complexes-of-copper-and-zinc-as-potential-anti-colitic-compounds
#1
Elaine M Conner, John Reglinski, W Ewen Smith, I Jack Zeitlin
The design, synthesis and activity of polymodal compounds for the treatment of inflammatory bowel disease are reported. The compounds, being based on a metal-Schiff base motif, are designed to degrade during intestinal transit to release the bioactive components in the gut. The compounds have been developed sequential with the biomodal compounds combining copper or zinc with a salicylaldehyde adduct. These compounds were tested in a formalin induced colonic inflammation model in BK:A mice. From these studies a trimodal compound based on a zinc Schiff base analogue of sulfasalazine was designed...
April 19, 2017: Biometals: An International Journal on the Role of Metal Ions in Biology, Biochemistry, and Medicine
https://www.readbyqxmd.com/read/28421991/patterns-in-use-and-costs-of-conventional-and-biologic-disease-modifying-anti-rheumatic-drugs-in-australia
#2
Ellen Donges, Christine Staatz, Helen Benham, Paul Kubler, Samantha A Hollingworth
OBJECTIVES: The aim of this study was to characterise the use and costs of subsidising conventional disease-modifying anti-rheumatic drugs (DMARDs) and biologic DMARDs in Australia from 2004-2014 through pharmaceutical benefits schemes. METHODS: Dispensing and expenditure data on conventional and biologic DMARDs were extracted from Medicare Australia and temporal trends were analysed. Medicine use was standardised in terms of the defined daily dose (DDD) per 1,000 population per day (DDD/1,000 population/day)...
April 18, 2017: Clinical and Experimental Rheumatology
https://www.readbyqxmd.com/read/28421826/6-gingerol-improves-testicular-function-in-mice-model-of-chronic-ulcerative-colitis
#3
E O Farombi, I A Adedara, B O Ajayi, T E Idowu, O O Eriomala, F O Akinbote
The persistent inflammation and oxidative stress at the local site in ulcerative colitis reportedly extend to the testes via systemic circulation resulting in testicular dysfunction. The influence of 6-gingerol (6G), a phenolic compound isolated from Zingiber officinale, on colitis-mediated testicular dysfunction in mice was investigated in this study. Chronic ulcerative colitis was induced in mice using 2.5% dextran sulfate sodium (DSS) in drinking water for three cycles. Each cycle consisted of 7 consecutive days of exposure to DSS-treated water followed by 14 consecutive days of normal drinking water...
January 1, 2017: Human & Experimental Toxicology
https://www.readbyqxmd.com/read/28412710/triple-oral-therapy-versus-antitumor-necrosis-factor-plus-methotrexate-mtx-in-patients-with-rheumatoid-arthritis-and-inadequate-response-to-mtx-a-systematic-literature-review
#4
Julia Mary, Michel De Bandt, Cédric Lukas, Jacques Morel, Bernard Combe
OBJECTIVE: For patients with rheumatoid arthritis (RA) who have an inadequate response to methotrexate (MTX), the relative effectiveness of the combination of conventional disease-modifying antirheumatic drugs (DMARD) compared with the combination of tumor necrosis factor (TNF) inhibitors and MTX, as second-line therapy, is uncertain. The aim of this study was to compare the efficacy and tolerance of triple oral DMARD therapy versus anti-TNF agents associated with MTX in patients with RA after MTX failure...
April 15, 2017: Journal of Rheumatology
https://www.readbyqxmd.com/read/28408210/the-organic-anion-transporting-peptide-oatp-2b1-is-localized-in-the-basolateral-membrane-of-the-human-jejunum-and-caco-2-monolayers
#5
Markus Keiser, Lars Kaltheuner, Charlotte Wildberg, Janett Müller, Markus Grube, Lars Ivo Partecke, Claus-Dieter Heidecke, Stefan Oswald
The organic anion transporting polypeptide (OATP) 2B1 which is ubiquitously expressed in the human body is assumed to play an important role in the cellular uptake of many drugs. While the expression and function of this SLC transporter is well characterized in the human liver, little is known about its localization and functional relevance in the intestine. Thus, it was the aim of this study to investigate its localization and function in the human jejunum and in the frequently used intestinal Caco-2 cell line...
April 10, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28388820/rheumatoid-arthritis-treatment-after-methotrexate-triple-therapy-is-more-durable-than-etanercept
#6
Shana M Peper, Robert Lew, Ted Mikuls, Mary Brophy, Denis Rybin, Hongseng Wu, James O'Dell
OBJECTIVE: Although it is common for rheumatologists to initiate biologics after failure of methotrexate monotherapy in rheumatoid arthritis (RA), ample data supports the initial use of combinations of conventional therapies in this clinical scenario. Our study explores the durability of triple therapy (methotrexate, sulfasalazine, and hydroxychloroquine) versus methotrexate-etanercept in RA. METHODS: RA patients with suboptimal response to methotrexate (n = 353) were randomized to either triple therapy or methotrexate-etanercept therapy in a 48-week, double-blinded, non-inferiority trial...
April 7, 2017: Arthritis Care & Research
https://www.readbyqxmd.com/read/28382174/cysteine-transporter-slc3a1-promotes-breast-cancer-tumorigenesis
#7
Yang Jiang, Yuan Cao, Yongbin Wang, Wei Li, Xinyi Liu, Yixuan Lv, Xiaoling Li, Jun Mi
Cysteine is an essential amino acid for infants, aged people as well as patients with metabolic disorders. Although the thiol group of cysteine side chain is active in oxidative reactions, the role of cysteine in cancer remains largely unknown. Here, we report that the expression level of the solute carrier family 3, member 1 (SLC3A1), the cysteine carrier, tightly correlated with clinical stages and patients' survival. Elevated SLC3A1 expression accelerated the cysteine uptake and the accumulation of reductive glutathione (GSH), leading to reduced reactive oxygen species (ROS)...
2017: Theranostics
https://www.readbyqxmd.com/read/28378336/review-of-treatment-for-alopecia-totalis-and-alopecia-universalis
#8
REVIEW
Sama Kassira, Dorota Z Korta, Lance W Chapman, Francis Dann
Alopecia areata (AA) is an autoimmune disease directed at the hair follicle. Although usually limited to patchy hair loss over the scalp (focalis), AA can present as total loss of scalp hair (totalis; AT) or as total loss of both scalp and body hair (universalis; AU). Management of AT and AU can be challenging, and although multiple treatment modalities have been explored, no therapy is currently FDA-approved. This review focuses on the evidence for current treatment options for AT and AU. The PubMed database was searched from January 1, 2000, to September 1, 2016, for clinical trials, retrospective studies, and case reports of treatments for AT and AU...
April 5, 2017: International Journal of Dermatology
https://www.readbyqxmd.com/read/28366005/evaluation-of-dissolution-in-the-lower-intestine-and-its-impact-on-the-absorption-process-of-high-dose-low-solubility-drugs
#9
Danai Georgaka, James Butler, Filippos Kesisoglou, Christos Reppas, Maria Vertzoni
PURPOSE: First, to optimize a recently proposed two-stage single-compartment in vitro test for the evaluation of dissolution in the lower intestine with the mini-paddle apparatus in the fasted and fed state using two model high dose, low solubility drugs [sulfasalazine (Azulfidine®) and micronized aprepitant] and one mesalamine colon targeting product (Asacol, 400mg/tablet). Second, to evaluate the impact of passive absorption from the lower intestine on the overall absorption process using three model high dose, low solubility drugs [micronized aprepitant, SB705498, and albendazole (Zentel®)]...
April 1, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28364659/an-in%C3%A2-vitro-and-in%C3%A2-vivo-evaluation-of-new-potential-trans-sialidase-inhibitors-of-trypanosoma-cruzi-predicted-by-a-computational-drug-repositioning-method
#10
Edgar E Lara-Ramirez, Julio Cesar López-Cedillo, Benjamin Nogueda-Torres, Muhammad Kashif, Carlos Garcia-Perez, Virgilio Bocanegra-Garcia, Rosalía Agusti, María Laura Uhrig, Gildardo Rivera
Chagas disease is one of the most important neglected parasitic diseases afflicting developed and undeveloped countries. There are currently limited options for inexpensive and secure pharmacological treatment. In this study, we employed a structure-based virtual screening protocol for 3180 FDA-approved drugs for repositioning of them as potential trans-sialidase inhibitors. In vitro and in vivo evaluations were performed for the selected drugs against trypomastigotes from the INC-5 and NINOA strains of T...
March 28, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28322941/small-dosing-clinical-study-pharmacokinetic-pharmacogenomic-slco2b1-and-abcg2-and-interaction-atorvastatin-and-grapefruit-juice-profiles-of-five-probes-for-oatp2b1-and-bcrp
#11
Yushi Kashihara, Ichiro Ieiri, Takashi Yoshikado, Maeda Kazuya, Masato Fukae, Miyuki Kimura, Takeshi Hirota, Shunji Matsuki, Shin Irie, Noritomo Izumi, Hiroyuki Kusuhara, Yuichi Sugiyama
The aims of this study were (1) to investigate the effects of atorvastatin (10 mg, therapeutic dose) and grapefruit juice (GFJ), inhibitors of OATP2B1, on the pharmacokinetics of substrates for OATP2B1 and BCRP under oral small-dosing conditions (300 μg sulfasalazine, 250 μg rosuvastatin, 300 μg glibenclamide, 1200 μg celiprolol, and 600 μg sumatriptan), and (2) to evaluate the contribution of SLCO2B1*3 and ABCG2 c.421C>A polymorphisms to the pharmacokinetics of the five test drugs in 23 healthy volunteers...
March 17, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28296755/inflammatory-bowel-diseases-a-burden-in-pediatrics-case-series-and-a-review-of-the-literature
#12
Cristina Oana Mărginean, Lorena Elena Meliţ, Simona Mocanu, Maria Oana Mărginean
INTRODUCTION: Inflammatory bowel disease is a chronic condition of the gastrointestinal tract, comprising mainly Crohn disease (CD) and ulcerative colitis (UC). Both of them are frequently encountered in children, being multifactorial conditions, with an unclear etiology. PATIENTS CONCERNS: We present 4 cases of inflammatory bowel disease (IBD) in children in order to underline the variable evolution depending on the patient's particularities. DIAGNOSIS, INTERVENTIONS AND OUTCOMES: The first case, a 13-year-old male patient, with a history of Henoch-Schonlein purpura, was admitted for rectal bleeding and weight loss, with normal laboratory parameters...
March 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28293446/real-life-experience-of-using-conventional-disease-modifying-anti-rheumatic-drugs-dmards-in-psoriatic-arthritis-psa-retrospective-analysis-of-the-efficacy-of-methotrexate-sulfasalazine-and-leflunomide-in-psa-in-comparison-to-spondyloarthritides-other-than-psa
#13
Euthalia Roussou, Aicha Bouraoui
OBJECTIVE: With the aim of assessing the response to treatment with conventional disease-modifying anti-rheumatic drugs (DMARDs) used in patients with psoriatic arthritis (PsA), data on methotrexate, sulfasalazine (SSZ), and leflunomide were analyzed from baseline and subsequent follow-up (FU) questionnaires completed by patients with either PsA or other spondyloarthritides (SpAs). MATERIAL AND METHODS: A single-center real-life retrospective analysis was performed by obtaining clinical data via questionnaires administered before and after treatment...
March 2017: European Journal of Rheumatology
https://www.readbyqxmd.com/read/28275295/investigation-of-mitigating-effect-of-colon-specific-prodrugs-of-boswellic-acid-on-2-4-6-trinitrobenzene-sulfonic-acid-induced-colitis-in-wistar-rats-design-kinetics-and-biological-evaluation
#14
Ajinkya Sarkate, Suneela S Dhaneshwar
AIM: To develop a colon-targeting bioreversible delivery system for β-boswellic acid (BBA) and explore utility of its prodrugs in 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitis in rats. METHODS: Synthesis of 4 co-drugs of BBA with essential amino acids was achieved by CDI coupling, followed by their spectral characterization. In vitro kinetics were studied by HPLC in aqueous buffers, homogenates of gastrointestinal tract and fecal matter. In vivo kinetic studies were performed in Wistar rat plasma, urine and feces...
February 21, 2017: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/28264816/eular-recommendations-for-the-management-of-rheumatoid-arthritis-with-synthetic-and-biological-disease-modifying-antirheumatic-drugs-2016-update
#15
Josef S Smolen, Robert Landewé, Johannes Bijlsma, Gerd Burmester, Katerina Chatzidionysiou, Maxime Dougados, Jackie Nam, Sofia Ramiro, Marieke Voshaar, Ronald van Vollenhoven, Daniel Aletaha, Martin Aringer, Maarten Boers, Chris D Buckley, Frank Buttgereit, Vivian Bykerk, Mario Cardiel, Bernard Combe, Maurizio Cutolo, Yvonne van Eijk-Hustings, Paul Emery, Axel Finckh, Cem Gabay, Juan Gomez-Reino, Laure Gossec, Jacques-Eric Gottenberg, Johanna M W Hazes, Tom Huizinga, Meghna Jani, Dmitry Karateev, Marios Kouloumas, Tore Kvien, Zhanguo Li, Xavier Mariette, Iain McInnes, Eduardo Mysler, Peter Nash, Karel Pavelka, Gyula Poór, Christophe Richez, Piet van Riel, Andrea Rubbert-Roth, Kenneth Saag, Jose da Silva, Tanja Stamm, Tsutomu Takeuchi, René Westhovens, Maarten de Wit, Désirée van der Heijde
Recent insights in rheumatoid arthritis (RA) necessitated updating the European League Against Rheumatism (EULAR) RA management recommendations. A large international Task Force based decisions on evidence from 3 systematic literature reviews, developing 4 overarching principles and 12 recommendations (vs 3 and 14, respectively, in 2013). The recommendations address conventional synthetic (cs) disease-modifying antirheumatic drugs (DMARDs) (methotrexate (MTX), leflunomide, sulfasalazine); glucocorticoids (GC); biological (b) DMARDs (tumour necrosis factor (TNF)-inhibitors (adalimumab, certolizumab pegol, etanercept, golimumab, infliximab), abatacept, rituximab, tocilizumab, clazakizumab, sarilumab and sirukumab and biosimilar (bs) DMARDs) and targeted synthetic (ts) DMARDs (Janus kinase (Jak) inhibitors tofacitinib, baricitinib)...
March 6, 2017: Annals of the Rheumatic Diseases
https://www.readbyqxmd.com/read/28261835/systematic-review-with-meta-analysis-use-of-5-aminosalicylates-and-risk-of-colorectal-neoplasia-in-patients-with-inflammatory-bowel-disease
#16
REVIEW
S Bonovas, G Fiorino, T Lytras, G Nikolopoulos, L Peyrin-Biroulet, S Danese
BACKGROUND: The relationship of 5-aminosalicylates' use with the risk of colorectal neoplasia in patients with inflammatory bowel disease (IBD) has been the focus of a growing body of research. AIM: To investigate this association through an updated meta-analysis of observational studies. METHODS: PubMed, Scopus and major conference proceedings were searched up to December 2016. The identified studies were evaluated for publication bias and heterogeneity...
May 2017: Alimentary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28260798/geniposide-ameliorates-tnbs-induced-experimental-colitis-in-rats-via-reducing-inflammatory-cytokine-release-and-restoring-impaired-intestinal-barrier-function
#17
Bin Xu, Yan-Li Li, Ming Xu, Chang-Chun Yu, Meng-Qiao Lian, Ze-Yao Tang, Chuan-Xun Li, Yuan Lin
Geniposide is an iridoid glycosides purified from the fruit of Gardenia jasminoides Ellis, which is known to have antiinflammatory, anti-oxidative and anti-tumor activities. The present study aimed to investigate the effects of geniposide on experimental rat colitis and to reveal the related mechanisms. Experimental rat colitis was induced by rectal administration of a TNBS solution. The rats were treated with geniposide (25, 50 mg·kg(-1)·d(-1), ig) or with sulfasalazine (SASP, 100 mg·kg(-1)·d(-1), ig) as positive control for 14 consecutive days...
March 6, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28253902/sulfasalazine-attenuates-evading-anticancer-response-of-cd133-positive-hepatocellular-carcinoma-cells
#18
Yeonhwa Song, Jaewoo Jang, Tae-Hoon Shin, Sang Mun Bae, Jin-Sun Kim, Kang Mo Kim, Seung-Jae Myung, Eun Kyung Choi, Haeng Ran Seo
BACKGROUND: CD133-positive cells in hepatocellular carcinoma (HCC) exhibit cancer stem cell (CSC)-like properties as well as resistance to chemotherapeutic agents and ionizing radiation; however, their function remains unknown. In this paper, we identified a hitherto unknown mechanism to overcome CD133-induced resistance to anticancer therapy. METHODS: We applied an alternative approach to enrich the CD133-positive HCC population by manipulating 3D culture conditions...
March 3, 2017: Journal of Experimental & Clinical Cancer Research: CR
https://www.readbyqxmd.com/read/28210090/efficacy-and-safety-of-stellate-ganglion-block-in-chronic-ulcerative-colitis
#19
Hong-Ying Zhao, Guo-Tao Yang, Ning-Ning Sun, Yu Kong, Yun-Feng Liu
AIM: To investigate the efficacy and safety of stellate ganglion block for the treatment of patients with chronic ulcerative colitis. METHODS: A total of 120 randomly selected patients with chronic ulcerative colitis treated in Cangzhou Central Hospital from January 2014 to January 2016 were included in this study. These patients were divided into two groups: control group (n = 30), patients received oral sulfasalazine treatment; experimental group (n = 90), patients received stellate ganglion block treatment...
January 21, 2017: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/28179619/rituximab-can-induce-remission-in-a-patient-with-ankylosing-spondylitis-who-failed-anti-tnf-%C3%AE-agent
#20
Fahmi AlDhaheri, Talal Almteri, Naji Dwid, Ahd Majdali, Nahed Janoudi, Hani Almoallim
BACKGROUND Ankylosing spondylitis (AS) is a chronic inflammatory disease that predominantly affects the axial skeleton. The ability of anti-TNF-α agents to reduce disease activity in patients with axial spondyloarthritis (axSpA), including AS, has been demonstrated in multiple randomized trials and several meta-analyses. Reports on the efficacy of rituximab in treatment of AS have described good results. We report on a patient with AS who failed anti-TNF-α therapy but showed good clinical improvement with rituximab therapy...
February 9, 2017: American Journal of Case Reports
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