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Colchicine

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https://www.readbyqxmd.com/read/27918450/janus-compounds-5-chloro-n%C3%A2-methyl-n%C3%A2-aryl-9h-pyrimido-4-5-b-indole-2-4-diamines-cause-both-microtubule-depolymerizing-and-stabilizing-effects
#1
Cristina C Rohena, April L Risinger, Ravi Kumar Vyas Devambatla, Nicholas F Dybdal-Hargreaves, Roma Kaul, Shruti Choudhary, Aleem Gangjee, Susan L Mooberry
While evaluating a large library of compounds designed to inhibit microtubule polymerization, we identified four compounds that have unique effects on microtubules. These compounds cause mixed effects reminiscent of both microtubule depolymerizers and stabilizers. Immunofluorescence evaluations showed that each compound initially caused microtubule depolymerization and, surprisingly, with higher concentrations, microtubule bundles were also observed. There were subtle differences in the propensity to cause these competing effects among the compounds with a continuum of stabilizing and destabilizing effects...
December 2, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27915168/interactions-of-long-chain-homologues-of-colchicine-with-tubulin
#2
Ana Marzo-Mas, Pascale Barbier, Gilles Breuzard, Diane Allegro, Eva Falomir, Juan Murga, Miguel Carda, Vincent Peyrot, J Alberto Marco
Several colchicine analogues in which the N-acetyl residue has been replaced by aliphatic, straight-chain acyl moieties, have been synthesized. These compounds show high cytotoxic activity at the nanomolar level against the tumoral cell lines HT-29, MCF-7 and A549. Some of them exhibit activities in the picomolar range against the HT-29 line and are thus two to three orders of magnitude more cytotoxic than colchicine. In this specific cell line, the activities were found to be closely related to the length of the acyl carbon chain, an increase in the latter giving rise to an increase in the cytotoxicity with a maximum in the range of 10-12 carbon atoms, followed by a decrease in activity with still longer chains...
November 23, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27912174/synthesis-and-cytostatic-properties-of-polyfunctionalized-furanoallocolchicinoids
#3
Iuliia A Gracheva, Iuliia V Voitovich, Vladimir I Faerman, Nikolay S Sitnikov, Ekaterina V Myrsikova, Hans-Gunther Schmalz, Elena V Svirshevskaya, Alexey Yu Fedorov
A series of furan-based allocolchicinoids was prepared from commercially available colchicine via a nine-step reaction sequence. Cytostatic activity, cell cycle arrest, apoptosis, tubulin and F-actin expression were studied in vitro in 2D and 3D cultures of normal and tumor epithelial keratinocytes, endothelial and mesenchymal cells. Among the prepared furanoallocolchicine analogues, 14a and 7a displayed the most pronounced anti-cancer activity. These compounds induced two types of effects: (a) cell cycle arrest in the G2/M phase as a direct consequence of effective tubulin binding (metaphase effect), and (b) pronounced cell stress (as evidenced by the overexpression of tubulin and F-actin), which was caused by the hyperpolarization of mitochondrial and lysosomal membranes (interphase effect)...
November 16, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27906774/lessons-from-characterization-and-treatment-of-the-autoinflammatory-syndromes
#4
Ivona Aksentijevich, Michael F McDermott
PURPOSE OF REVIEW: The list of genes associated with systemic inflammatory diseases has been steadily growing because of the explosion of new genomic technologies. Significant advances in the past year have deepened our understanding of the molecular mechanisms linked to inflammation and elucidated insights on the efficacy of specific therapies for these and related conditions. We review the molecular pathogenesis of four recently characterized monogenic autoinflammatory diseases: haploinsufficiency of A20, otulipenia, a severe form of pyrin-associated disease, and a monogenic form of systemic juvenile idiopathic arthritis...
November 30, 2016: Current Opinion in Rheumatology
https://www.readbyqxmd.com/read/27899171/the-effects-of-melatonin-and-colchicine-on-ischemia-reperfusion-injury-in-experimental-rat-testicular-torsion-model
#5
Tamer Sekmenli, Metin Gunduz, Bahadır Öztürk, Pınar Karabağlı, Ilhan Ciftci, Gülsüm Tekin, Mustafa Yılmaz
PURPOSE: The aim of the present study is to investigate the efficiency of colchicine and melatonın in an experimental rat testicular torsion model in the light of histological and biochemical data. METHODS: A total of 34 Wistar albino male rats were randomly divided into 5 groups as: Group C (control, n=6), Group S (sham; underwent only left scrotal exploration, n=7), Group TD (torsion and detorsion; 6h of ischemia and 7days of reperfusion, n=7), Group TD/M (TD+Melatonin; 6h of ischemia and 7days of reperfusion and 7days of 17mg/kg intraperitoneal melatonin per day, n=7), group TD/Col (TD+Colchicine; 6h of ischemia and 7days of reperfusion and 7days of 1mg/kg oral colchicine per day, n=7)...
November 18, 2016: Journal of Pediatric Surgery
https://www.readbyqxmd.com/read/27895581/evaluation-of-near-infrared-dyes-as-markers-of-p-glycoprotein-activity-in-tumors
#6
Inessa Semenenko, Emma Portnoy, Mohammed Aboukaoud, Serge Guzy, Miriam Shmuel, Gal Itzhak, Sara Eyal
Aim: The multidrug resistance protein 1 (MDR1; P-glycoprotein) has been associated with efflux of chemotherapeutic agents from tumor cells and with poor patient prognosis. This study evaluated the feasibility of non-invasive, non-radioactive near infrared (NIR) imaging methodology for detection of MDR1 functional activity in tumors. Methods: Initial accumulation assays were conducted in MDR1-overexpressing MDCK cells (MDCK-MDR1) and control MDCK cells (MDCK-CT) using the NIR dyes indocyanine green (ICG), IR-783, IR-775, rhodamine 800, XenoLight DiR, and Genhance 750, at 0...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27894589/discovery-and-preclinical-evaluation-of-7-benzyl-n-substituted-pyrrolo-3-2-d-pyrimidin-4-amines-as-single-agents-with-microtubule-targeting-effects-along-with-triple-acting-angiokinase-inhibition-as-antitumor-agents
#7
Roheeth Kumar Pavana, Shruti Choudhary, Anja Bastian, Michael A Ihnat, Ruoli Bai, Ernest Hamel, Aleem Gangjee
The utility of cytostatic antiangiogenic agents (AA) in cancer chemotherapy lies in their combination with cytotoxic chemotherapeutic agents. Clinical combinations of AA with microtubule targeting agents (MTAs) have been particularly successful. The discovery, synthesis and biological evaluations of a series of 7-benzyl-N-substituted-pyrrolo[3,2-d]pyrimidin-4-amines are reported. Novel compounds which inhibit proangiogenic receptor tyrosine kinases (RTKs) including vascular endothelial growth factor receptor-2 (VEGFR-2), platelet-derived growth factor receptor-β (PDGFR-β) and epidermal growth factor receptor (EGFR), along with microtubule targeting in single molecules are described...
November 15, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27886801/approach-to-the-patients-with-inadequate-response-to-colchicine-in-familial-mediterranean-fever
#8
REVIEW
Ahmet Gül
Familial Mediterranean fever (FMF) is the most common form of monogenic autoinflammatory conditions, and response to colchicine has been considered as one of its distinctive features among other hereditary periodic fever disorders. Prophylactic colchicine has been shown to be effective in the prevention of inflammatory attacks and development of amyloidosis. However, the highest tolerable doses of colchicine may not be adequate enough to manage these goals in approximately 5% of FMF patients. Inadequate response to colchicine in fully compliant FMF patients may be associated with genetic and/or environmental factors affecting disease severity and colchicine bioavailability...
April 2016: Best Practice & Research. Clinical Rheumatology
https://www.readbyqxmd.com/read/27884251/complicated-pericarditis-understanding-risk-factors-and-pathophysiology-to%C3%A2-inform%C3%A2-imaging-and-treatment
#9
REVIEW
Paul C Cremer, Arnav Kumar, Apostolos Kontzias, Carmela D Tan, E Rene Rodriguez, Massimo Imazio, Allan L Klein
Most patients with acute pericarditis have a benign course and a good prognosis. However, a minority of patients develop complicated pericarditis, and the care of these patients is the focus of this review. Specifically, we address risk factors, multimodality imaging, pathophysiology, and novel treatments. The authors conclude that: 1) early high-dose corticosteroids, a lack of colchicine, and an elevated high-sensitivity C-reactive protein are associated with the development of complicated pericarditis; 2) in select cases, cardiovascular magnetic resonance imaging may aid in the assessment of pericardial inflammation and constriction; 3) given phenotypic similarities between recurrent idiopathic pericarditis and periodic fever syndromes, disorders of the inflammasome may contribute to relapsing attacks; and 4) therapies that target the inflammasome may lead to more durable remission and resolution...
November 29, 2016: Journal of the American College of Cardiology
https://www.readbyqxmd.com/read/27875029/decreased-activity-and-genetic-polymorphisms-of-cyp2c19-in-beh%C3%A3-et-s-disease
#10
Mustafa Tugrul Goktas, R Ozgur Karaca, Said Kalkisim, Lokman Cevik, Levent Kilic, Ali Akdogan, Melih O Babaoglu, Atilla Bozkurt, Leif Bertilsson, Umit Yasar
Behçet's disease (BD) is a systemic autoimmune disorder. Cytochrome P450 enzymes (CYPs) are responsible for various drug metabolism reactions as well as those of endogenous substances which may be associated with autoimmune disease susceptibility. Recently, we reported that in patients with BD, CYP2C9 seems to be down-regulated due to inflammation. In the same Turkish BD patients, we investigated whether also CYP2C19 activity is decreased. Lansoprazole (30 mg) was given as a probe drug to evaluate CYP2C19 activity in 59 patients with BD and 27 healthy control volunteers...
November 22, 2016: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/27874260/phototriggered-secretion-of-membrane-compartmentalized-bioactive-agents
#11
Robert M Hughes, Christina M Marvin, Zachary L Rodgers, Song Ding, Nathan P Oien, Weston J Smith, David S Lawrence
A strategy for the light-activated release of bioactive compounds (BODIPY, colchicine, paclitaxel, and methotrexate) from membrane-enclosed depots is described. We have found that membrane-permeable bioagents can be rendered membrane impermeable by covalent attachment to cobalamin (Cbl) through a photocleavable linker. These Cbl-bioagent conjugates are imprisoned within lipid-enclosed compartments in the dark, as exemplified by their retention in the interior of erythrocytes. Subsequent illumination drives the secretion of the bioactive species from red blood cells...
November 22, 2016: Angewandte Chemie
https://www.readbyqxmd.com/read/27867744/iga-pemphigus-showing-iga-antibodies-to-desmoglein-1-and-3
#12
Salama Hegazy, Sana Bouchouicha, Aida Khaled, Lilia Laadher, Maryem Kallel Sellami, Faten Zeglaoui
BACKGROUND: IgA pemphigus is a rare autoimmune vesiculo-pustular skin disease. Only approximately 70 cases have been reported to date. We report a case of IgA pemphigus with IgA antibodies to desmoglein 1 (Dsg1) and desmoglein 3 (Dsg3). CASE REPORT: We report the case of an 60-year-old man with intraepidermal neutrophilic IgA pemphigus with IgA antibodies to Dsg1 and Dsg3. Histologic examination revealed subcorneal neutrophilic pustules with few acantholytic cells...
October 2016: Dermatology Practical & Conceptual
https://www.readbyqxmd.com/read/27862994/colchicine-increases-ventricular-vulnerability-in-an-experimental-whole-heart-model
#13
Gerrit Frommeyer, Julius Krawczyk, Dirk G Dechering, Simon Kochhäuser, Patrick Leitz, Michael Fehr, Lars Eckardt
The traditional gout medication colchicine has been reported to effectively prevent atrial fibrillation recurrence after atrial fibrillation ablation or cardiac surgery in a few clinical trials. Severe adverse events have not yet been reported. The aim of the present study was to assess possible direct electrophysiological effects in an experimental whole-heart model. Ten rabbit hearts were isolated and Langendorff-perfused. Thereafter, colchicine was administered in 2 concentrations (1μM and 3μM). Eight endo- and epicardial monophasic action potentials and a 12-lead ECG showed a stable QT interval and action potential duration during colchicine infusion...
November 11, 2016: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/27860460/anakinra-for-colchicine-resistant-familial-mediterranean-fever-a-randomized-double-blind-placebo-controlled-trial
#14
Ilan Ben-Zvi, Olga Kukuy, Eitan Giat, Elon Pras, Olga Feld, Shaye Kivity, Senior Lecturer, Oleg Perski, Gil Bornstein, Chagai Grossman, Gil Harari, Merav Lidar, Avi Livneh
Objective - Familial Mediterranean fever (FMF) is refractory to colchicine prophylaxis in 10-20% of patients. A patient series showed anakinra, an IL-1 blocking agent, to prevent FMF attacks in colchicine-resistant FMF (CRFMF). Here we studied the efficacy and safety of anakinra in the treatment of CRFMF, using a randomized controlled trial. Methods - CRFMF patients receiving colchicine (≥1.5 to ≤3 mg/day) were recruited and randomly assigned to receive anakinra or placebo (vehicle). Treatment duration was 4 months...
November 11, 2016: Arthritis & Rheumatology
https://www.readbyqxmd.com/read/27860168/use-of-a-350-mm-2-baerveldt-glaucoma-drainage-device-to-maintain-vision-and-control-intraocular-pressure-in-dogs-with-glaucoma-a-retrospective-study-2013-2016
#15
Kathleen L Graham, David Donaldson, Francis A Billson, F Mark Billson
OBJECTIVE: To evaluate the 350-mm(2) Baerveldt glaucoma drainage device (GDD) in dogs with refractory glaucoma when modifications to address postoperative hypotony (extraluminal ligature; intraluminal stent) and the fibroproliferative response (intraoperative Mitomycin-C; postoperative oral colchicine and prednisolone) are implemented as reported in human ophthalmology. DESIGN: Retrospective case series. ANIMALS: Twenty-eight client-owned dogs (32 eyes) including seven dogs (nine eyes) with primary glaucoma and 21 dogs (23 eyes) with secondary glaucoma...
November 16, 2016: Veterinary Ophthalmology
https://www.readbyqxmd.com/read/27834133/the-effects-of-colchicum-baytopiorum-on-regulatory-genes-of-apoptotic-and-autophagic-cell-death-in-hela-cells
#16
Özlem D Özsöylemez, Melek Öztürk, Nurhayat Sütlüpinar, Sera Kayacan, Matem Tunçdemir, Gül Özcan
BACKGROUND: The natural products have increasing important for the development of anticancer agents. Colchicum baytopiorum C.D.Brickell (C. baytopiorum), an endemic species for Turkey, contains colchicine and its derivatives. Stimulation of apoptotic and autophagy-mediated cell deaths are effective strategy for anticancer therapies. AIM: The aim of the study is to determine the role of the extract on both apoptotic and autophagic cell death in HeLa cell line. METHODS: The cell viability of C...
November 9, 2016: Current Pharmaceutical Biotechnology
https://www.readbyqxmd.com/read/27832960/novel-indole-based-compounds-that-differentiate-alkylindole-sensitive-receptors-from-cannabinoid-receptors-and-microtubules-characterization-of-their-activity-on-glioma-cell-migration
#17
Susan Fung, Cong Xu, Ernest Hamel, James B Wager-Miller, Grace Woodruff, Aaron Miller, Christina Sanford, Ken Mackie, Nephi Stella
Indole-based compounds, such as the alkyl-indole (AI) compound WIN55212-2, activate the cannabinoid receptors, CB1 and CB2, two well-characterized G protein-coupled receptors (GPCR). Reports indicate that several indole-based cannabinoid agonists, including WIN55212-2, lack selectivity and interact with at least two additional targets: AI-sensitive GPCRs and microtubules. Studying how indole-based compounds modulate the activity of these 4 targets has been difficult as selective chemical tools were not available...
November 7, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27825009/effect-of-anakinra-on-recurrent-pericarditis-among-patients-with-colchicine-resistance-and-corticosteroid-dependence-the-airtrip-randomized-clinical-trial
#18
Antonio Brucato, Massimo Imazio, Marco Gattorno, George Lazaros, Silvia Maestroni, Mara Carraro, Martina Finetti, Davide Cumetti, Alessandra Carobbio, Nicolino Ruperto, Renzo Marcolongo, Monia Lorini, Alessandro Rimini, Anna Valenti, Gian Luca Erre, Maria Pia Sormani, Riccardo Belli, Fiorenzo Gaita, Alberto Martini
Importance: Anakinra, an interleukin 1β recombinant receptor antagonist, may have potential to treat colchicine-resistant and corticosteroid-dependent recurrent pericarditis. Objective: To determine the efficacy of anakinra for colchicine-resistant and corticosteroid-dependent recurrent pericarditis. Design, Setting, and Participants: The Anakinra-Treatment of Recurrent Idiopathic Pericarditis (AIRTRIP) double-blind, placebo-controlled, randomized withdrawal trial (open label with anakinra followed by a double-blind withdrawal step with anakinra or placebo until recurrent pericarditis occurred) conducted among 21 consecutive patients enrolled at 3 Italian referral centers between June and November 2014 (end of follow-up, October 2015)...
November 8, 2016: JAMA: the Journal of the American Medical Association
https://www.readbyqxmd.com/read/27823912/-chronic-recurrent-annular-neutrophilic-dermatosis
#19
A Croci-Torti, B Guillot, V Rigau, D Bessis
BACKGROUND: Chronic recurrent annular neutrophilic dermatosis (CRAND) is a rare form of neutrophilic dermatosis characterised by chronic annular progression, histological impairment similar to that seen in Sweet's syndrome and the absence of association with generalised signs, abnormal laboratory values or underlying systemic disease. Herein we report two new cases. PATIENTS AND METHODS: Case n(o) 1. A 41-year-old woman had presented with four annular lesions on the forearms and neckline which she had had for one year...
November 4, 2016: Annales de Dermatologie et de Vénéréologie
https://www.readbyqxmd.com/read/27823884/synthesis-structure-activity-relationships-and-biological-evaluation-of%C3%A2-7-phenyl-pyrroloquinolinone-3-amide-derivatives-as-potent-antimitotic-agents
#20
Davide Carta, Roberta Bortolozzi, Mattia Sturlese, Veronica Salmaso, Ernest Hamel, Giuseppe Basso, Laura Calderan, Luigi Quintieri, Stefano Moro, Giampietro Viola, Maria Grazia Ferlin
A small library of 7-pyrrolo[3,2-f]quinolinones was obtained by introducing benzoyl, sulfonyl and carbamoyl side chains at the 3-N position, and their cytotoxicity against a panel of leukemic and solid tumor cell lines was evaluated. Most of them showed high antiproliferative activity with GI50s ranging from micro-to sub-nanomolar values, and these values correlated well with the inhibitory activities of the compounds against tubulin polymerization. Based on a recently proposed colchicine bind site inhibitors (CBSIs) pharmacophore, the interactions of the novel 7-PPyQs at the colchicine domain were rationalized...
October 21, 2016: European Journal of Medicinal Chemistry
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