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Colchicine

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https://www.readbyqxmd.com/read/29232311/lithium-colchicine-a-potential-strategy-to-reduce-pro-inflammatory-effects-of-lithium-treatment
#1
John J Mooney, Roscoe O Brady
PURPOSE: Rosenblat and McIntyre (Acta Psychiatr Scand. 2015;132: 180-191) propose that immune disorders are important mediators between bipolar disorders and medical comorbidities. Rosenblat et al (Bipolar Disord. 2016;18:89-101) present a meta-analysis showing that adjunctive anti-inflammatory agents could evoke moderate antidepressant responses in bipolar disorders. We propose using the anti-inflammatory drug colchicine to improve the long-term safety and efficacy of lithium treatment for bipolar disorders...
December 11, 2017: Journal of Clinical Psychopharmacology
https://www.readbyqxmd.com/read/29231948/a-tailored-nanosheet-decorated-with-a-metallized-dendrimer-for-angiography-and-magnetic-resonance-imaging-guided-combined-chemotherapy
#2
Guilong Zhang, Ruohong Du, Junchao Qian, Xiaojia Zheng, Xiaohe Tian, Dongqing Cai, Jiacai He, Yiqun Wu, Wei Huang, Yuanyin Wang, Xin Zhang, Kai Zhong, Duohong Zou, Zhengyan Wu
Considering the chemical exchange between gadolinium centers and water protons, nanosystems comprising gadolinium conjugated with high specific area nanocarriers might serve as more robust clinical tools for diagnosis and imaging-guided therapy. Herein, a pH-responsive nanosystem containing graphene oxide conjugated with a folic acid- and gadolinium-labeled dendrimer (FA-GCGLD) to boost its T1 contrast ability was developed, and doxorubicin (DOX) and colchicine (COLC) were efficiently loaded onto this nanosystem (FA-GCGLD-DOX/COLC)...
December 12, 2017: Nanoscale
https://www.readbyqxmd.com/read/29227648/quinazolinone-based-anticancer-agents-synthesis-anti-proliferative-sar-anti-tubulin-activity-and-tubulin-co-crystal-structure
#3
Wolfgang Dohle, Fabrice L Jourdan, Gregory Menchon, Andrea E Prota, Paul A Foster, Pascoe Mannion, Ernest Hamel, Mark P Thomas, Philip G Kasprzyk, Eric Ferrandis, Michel O Steinmetz, Mathew P Leese, Barry V L Potter
Quinazolinone-based anti-cancer agents were designed, decorated with functional groups from a 2-methoxyestradiol-based microtubule disruptor series, incorporating the aryl sulfamate motif of steroid sulfatase (STS) inhibitors. The steroidal AB-ring system was mimicked, favoring conformations with an N-2 substituent occupying D-ring space. Evaluation against breast and prostate tumor cell lines identified 7b with DU-145 anti-proliferative activity (GI50 300 nM). A preliminary structure-activity relationship afforded compounds (e...
December 11, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29223097/recent-advances-in-microtubule-stabilizing-agents
#4
REVIEW
Ya-Nan Cao, Ling-Li Zheng, Dan Wang, Xiao-Xia Liang, Feng Gao, Xian-Li Zhou
Highly dynamic mitotic spindle microtubules are superb therapeutic targets for a group of chemically diverse and clinically successful anticancer drugs. Microtubule-targeted drugs disrupt microtubule dynamics in distinct ways, and they are primarily classified into two groups: microtubule destabilizing agents (MDAs), such as vinblastine, colchicine, and combretastatin-A4, and microtubule stabilizing agents (MSAs), such as paclitaxel and epothilones. Systematic discovery and development of new MSAs have been aided by extensive research on paclitaxel, yielding a large number of promising anticancer compounds...
November 24, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29222636/identification-introgression-and-molecular-marker-genetic-analysis-and-selection-of-a-highly-effective-novel-oat-crown-rust-resistance-from-diploid-oat-avena-strigosa
#5
Howard W Rines, Marisa E Miller, Martin Carson, Shiaoman Chao, Tyler Tiede, Jochum Wiersma, Shahryar F Kianian
Oat crown rust is one of the most damaging diseases of oat. We identified a new source of resistance and developed KASP and TaqMan markers for selection in breeding programs. A new highly effective resistance to oat crown rust (Puccinia coronata f. sp. avenae) was identified in the diploid oat Avena strigosa PI 258731 and introgressed into hexaploid cultivated oat. Young plants with this resistance show moderate susceptibility, whereas older plant tissues and adult plants are resistant with no virulent isolates encountered in over 8 years of testing...
December 6, 2017: TAG. Theoretical and Applied Genetics. Theoretische und Angewandte Genetik
https://www.readbyqxmd.com/read/29220790/2-alkoxycarbonyl-3-arylamino-5-substituted-thiophenes-as-a-novel-class-of-antimicrotubule-agents-design-synthesis-cell-growth-and-tubulin-polymerization-inhibition
#6
Romeo Romagnoli, Maria Kimatrai Salvador, Santiago Schiaffino Ortega, Pier Giovanni Baraldi, Paola Oliva, Stefania Baraldi, Luisa Carlota Lopez-Cara, Andrea Brancale, Salvatore Ferla, Ernest Hamel, Jan Balzarini, Sandra Liekens, Elena Mattiuzzo, Giuseppe Basso, Giampietro Viola
Microtubules are recognized as crucial components of the mitotic spindle during cell division, and, for this reason, the microtubule system is an attractive target for the development of anticancer agents. Continuing our search strategy for novel tubulin targeting-compounds, a new series of 2-alkoxycarbonyl-3-(3',4',5'-trimethoxyanilino)-5-aryl/heteroarylthiophene derivatives was designed, synthesized and demonstrated to act as tubulin polymerization inhibitors at the colchicine site. A structure-activity relationship study on the phenyl at the 5-position of the thiophene ring was performed by introducing a variety of substituents containing electron-releasing and electron-withdrawing groups, with the 2-alkoxycarbonyl-3-(3',4',5'-trimethoxyanilino)thiophene scaffold being the minimum structural requirement for activity...
December 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29217970/recurrent-pericarditis-a-case-report-and-literature-review
#7
Justina Katinaitė, Birutė Petrauskienė
Background: Recurrence affects about 30% (20% to 50%) of patients within 18 months after the initial episode of acute pericarditis resulting in subsequent rehospitalizations. Bearing in mind high treatment costs of patients admitted to hospital with acute and recurrent pericarditis, there is a need to optimize the treatment of both of these conditions. Materials and methods: We present a case of recurrent pericarditis. The first episode of pericarditis was diagnosed in 2006...
2017: Acta Medica Lituanica
https://www.readbyqxmd.com/read/29215079/design-and-synthesis-of-5-aryl-4-4-arylpiperazine-1-carbonyl-2h-1-2-3-triazole-derivatives-as-colchicine-binding-site-inhibitors
#8
Yue Wu, Dongjie Feng, Meiqi Gao, Zhiwei Wang, Peng Yan, Zhenzhen Gu, Qi Guan, Daiying Zuo, Kai Bao, Jun Sun, Yingliang Wu, Weige Zhang
A series of 5-aryl-4-(4-arylpiperazine-1-carbonyl)-2H-1,2,3-triazol derivatives were designed as potential microtubule targeting agents. The regioselective alkylation of 5-aryl-4-(4-arylpiperazine-1-carbonyl)-2H-1,2,3-triazole was predicted by computations and confirmed by an unambiguous synthetic route. The antiproliferative activity of the synthesized compounds was tested in vitro using three human cancer cell lines and some compounds exhibited significant antiproliferative activity, which suggested the reasonability of introduction of the 1,2,3-triazole fragment...
December 7, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29214791/a-case-of-schnitzler-s-syndrome-without-monoclonal-gammopathy-associated-chronic-urticaria-treated-with-anakinra
#9
Min Joo Ahn, Ji Eun Yu, Jiung Jeong, Da Woon Sim, Young Il Koh
Chronic urticaria may often be associated with interleukin (IL)-1-mediated autoinflammatory disease, which should be suspected if systemic inflammation signs are present. Here, we report a case of Schnitzler's syndrome without monoclonal gammopathy treated successfully with the IL-1 receptor antagonist anakinra. A 69-year-old man suffered from a pruritic urticarial rash for 12 years. It became aggravated episodically and was accompanied by high fever, arthralgia, leukocytosis, and an elevated C-reactive protein and erythrocyte sedimentation rate...
January 2018: Yonsei Medical Journal
https://www.readbyqxmd.com/read/29214511/managing-gout-flares-in-the-elderly-practical-considerations
#10
Abhishek Abhishek
Gout is common in the elderly, affecting an estimated 4.7 million people aged > 60 years in the USA alone. The incidence and prevalence of gout increases, and male predisposition to gout reduces, with increasing age. The elderly have more comorbidities, and gout manifests differently, with more frequent involvement of knees, ankles, and wrists at disease onset, systemic upset, and tophi. Comorbidities and polypharmacy make the management of gout flares challenging in this population. Intra-articular corticosteroid injection remains the treatment of choice for accessible joints, oral prednisolone is preferred over low-dose colchicine, and non-steroidal anti-inflammatory drugs (NSAIDs) are best avoided...
December 6, 2017: Drugs & Aging
https://www.readbyqxmd.com/read/29214230/cytotoxicity-of-endocytosis-and-efflux-inhibitors-in-the-bewo-cell-line
#11
Mansi Shah, Luke Bourner, Shariq Ali, Sanaalarab Al-Enazy, Erik Rytting
Aims: The purpose of this study was to determine the cell viability and cytotoxicity of various endocytosis and efflux inhibitors which can be used to determine transport and uptake mechanisms in the BeWo (b30 clone) human placental trophoblast cell line. Ethanol and dimethylsulfoxide (DMSO) were also studied since they are often used as cosolvents for administration of these inhibitors. Methodology: The water-soluble tetrazolium-1 (WST-1) assay was used to quantify cell viability and the lactate dehydrogenase (LDH) assay was used to determine cytotoxicity...
2017: Journal of Pharmaceutical Research International
https://www.readbyqxmd.com/read/29207945/meningococcal-arthritis-and-myopericarditis-a-case-report
#12
Lloyd Steele, Katie Bechman, Eoghan De Barra, Charles Mackworth-Young
BACKGROUND: We report the first adult case of Neisseria meningitidis W-135 presenting with meningococcal arthritis and myopericarditis concomitantly, without other classical features of meningococcal disease. CASE PRESENTATION: A 67-year-old Caucasian man presented with acute-onset polyarthralgia, myalgia, and fever. On examination he had polyarticular synovitis. An electrocardiogram (ECG) demonstrated ST-elevation in leads I, II, III, aVF, and V2-V6 without reciprocal depression, and a high-sensitivity troponin level was significantly elevated...
December 6, 2017: BMC Infectious Diseases
https://www.readbyqxmd.com/read/29205989/postpericardiotomy-syndrome
#13
Joonas Lehto, Juha Virolainen
Postpericardiotomy syndrome (PPS) is a common complication following cardiac surgery. In most cases it develops 2 to 3 weeks after the operation. An inflammatory reaction develops in the pericardium or pleural space with fever, chest pain and dyspnea as typical symptoms. The disease process is usually self-limiting. At present, the etiology is unknown, but an immunological mechanism is suspected as the cause of the disease. The incidence of PPS is essentially dependent on diagnostic criteria, patient group and type of operation...
2017: Duodecim; Lääketieteellinen Aikakauskirja
https://www.readbyqxmd.com/read/29205987/recurrent-pericarditis
#14
Jukka Lehtonen
Recurrent pericarditis is the most common and problematic complication of acute pericarditis. After acute pericarditis, the pericarditis recurs in 20 to 50% of the patients. In most cases the etiology of pericarditis remains unclear, although it is generally thought to arise by an immunological mechanism. NSAID medication in combination with colchicine is the cornerstone of the treatment. Corticosteroids should be used mainly for those in whom the first-line drug treatment is not sufficient or first-line treatments are contraindicated...
2017: Duodecim; Lääketieteellinen Aikakauskirja
https://www.readbyqxmd.com/read/29205986/acute-pericarditis
#15
Ville Kytö, Matti Matti Niemelä
Acute pericarditis is typically associated with a viral infection. Chest pain appearing in connection with or soon after the symptoms of infection is the characteristic symptom. Diagnosis is based on the recognition of two characteristic findings (pericardial chest pain, pericardial friction rub, new ECG changes or new pericardial effusion). Medication with an anti-inflammatory analgesic for 1 to 2 weeks is the first-line treatment. A longer course of colchicine is recommended for the prevention of recurrence of the disease...
2017: Duodecim; Lääketieteellinen Aikakauskirja
https://www.readbyqxmd.com/read/29202409/a-fluorine-scan-of-a-tubulin-polymerization-inhibitor-isocombretastatin-a-4-design-synthesis-molecular-modelling-and-biological-evaluation
#16
Timothée Naret, Jérôme Bignon, Guillaume Bernadat, Mohamed Benchekroun, Helene Levaique, Christine Lenoir, Joelle Dubois, Alain Pruvost, François Saller, Delphine Borgel, Boris Manoury, Veronique Leblais, Romain Darrigrand, Sébastien Apcher, Jean-Daniel Brion, Etienne Schmitt, Frédéric R Leroux, Mouad Alami, Abdallah Hamze
A novel series of tubulin polymerization inhibitors, based on fluorinated derivatives of isocombretastatin A-4 was synthesized with the goal of evaluating the effect of these compounds on the proliferative activity. The introduction of fluorine atom was performed on the phenyl ring or at the linker between the two aromatic rings. The modification of isoCA-4 by introduction of difluoromethoxy group at the para-position (3i) and substitution of the two protons of the linker by two fluorine atoms (3m), produced the most active compounds in the series, with IC50 values of 0...
December 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29201931/colchicine-induced-hepatotoxicity
#17
Collette E Abbott, Ruliang Xu, Samuel H Sigal
Drug-induced injury (DILI) is a frequent cause of abnormal liver tests and a leading cause of liver failure in the United States. Colchicine has long been used as a systemic anti-inflammatory agent for treatment of gout by inhibiting mitotic activity and neutrophil function. We present the first case of colchicine-induced hepatoxicity, supported by histopathologic findings characteristic of colchicine-induced injury and resolution of liver enzyme abnormalities after its discontinuation. Colchicine-associated DILI has implications for the evaluation of patients with abnormal liver tests and gout, especially for patients with alcoholism and non-alcoholic fatty liver disease, in whom there is an increased incidence of gout...
2017: ACG Case Reports Journal
https://www.readbyqxmd.com/read/29201088/evaluation-of-a-99mtc-tricine-vascular-disrupting-agent-as-an-in-vivo-imaging-in-4t1-mouse-breast-tumor-model
#18
Mostafa Erfani, Seyed Pezhman Shirmardi, Mohammad Shafiei
Colchicine as a vascular disrupting agent creates microtubule destabilization which induces vessel blockage and consequently cell death. Accordingly, colchicines and its analogues radiolabeled with 99mTc may have potential for visualization of tumor. In this work, deacetylcolchicine a colchicine analogue was labeled with 99mTc via tricine as a coligand and characterized for its tumor targeting properties. The in-vitro radiochemical stability and the biodistribution were studied in 4T1 breast tumor model bearing mice...
2017: Iranian Journal of Pharmaceutical Research: IJPR
https://www.readbyqxmd.com/read/29200827/severe-hypertriglyceridemia-and-colchicine-intoxication-following-suicide-attempt
#19
Shaul Lev, David Snyder, Carmil Azran, Victor Zolotarsky, Arik Dahan
Colchicine overdose is uncommon but potentially life threatening. Due to its serious adverse systemic effects, overdose must be recognized and treated. We report a case of an 18-year-old female who ingested 18 mg (~0.4 mg/kg) of colchicine in a suicide attempt. The patient's clinical manifestations included abdominal cramps, vomiting, pancytopenia, hypocholesterolemia, and rhabdomyolysis. Two unique manifestations of toxicity in this patient were profound and persistent, severe hypertriglyceridemia and electrolyte imbalance, mainly hypophosphatemia, with no other evident cause except the colchicine intoxication...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29198919/does-colchicine-decrease-the-rate-of-recurrence-of-acute-idiopathic-pericarditis-treated-with-glucocorticoids
#20
Aviv Mager, Yeela Talmor, Chava Chezar Azzerad, Zaza Iakobishvili, Avital Porter, Ran Kornowski, David Hasdai
BACKGROUND: The traditional treatment of acute pericarditis includes non-steroidal anti-inflammatory agents (NSAIDs) or glucocorticoids. The addition of colchicine has been found to reduce the rate of recurrences. Glucocorticoids, however, may attenuate this effect, although the available data are limited. We examined the impact of colchicine on the rate of recurrence of acute idiopathic pericarditis pretreated with prednisone. METHODS: The frequency of recurrence in patients hospitalized for acute idiopathic pericarditis in a tertiary medical center in 2004-2014 who were treated with glucocorticoids or with non-steroidal therapy was assessed from the computerized hospital database...
November 30, 2017: Journal of Cardiology
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