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Colchicine

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https://www.readbyqxmd.com/read/28079286/design-synthesis-biological-evaluation-and-3d-qsar-analysis-of-podophyllotoxin-dioxazole-combination-as-tubulin-targeting-anticancer-agents
#1
Zi-Zhen Wang, Wen-Xue Sun, Xue Wang, Ya-Han Zhang, Han-Yue Qiu, Jin-Liang Qi, Yan-Jun Pang, Gui-Hua Lu, Xiao-Ming Wang, Fu-Gen Yu, Yong-Hua Yang
The advancement of cancer fighting drugs has never been a simple linear process. Those drugs design professionals begin to find inspiration from the nature after failing to find the ideal products by creative drugs design and high-throughput screening. To obtain new molecules for inhibiting tubulin, podophyllotoxin was adopted as the leading compound and 1,3,4-oxadiazole was brought in to the C-4 site of podophyllotoxin in this research. A series of seventeen podophyllotoxin derived esters have been achieved and then evaluated their antitumor activities against four different cancer cell lines: A549, MCF-7, HepG2 and HeLa...
January 12, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28079270/treatment-of-adults-with-idiopathic-recurrent-pericarditis-novel-use-of-immunotherapy
#2
Nicholas C Schwier, Genevieve Hale, Marie L Davies
Idiopathic recurrent pericarditis (IRP) can be challenging to treat. Even after guideline-directed, first-line treatment consisting of aspirin (ASA) or a nonsteroidal antiinflammatory drug (NSAID) in combination with colchicine therapy, recurrences still occur in greater than 20% of patients. Many patients then require treatment with long-term corticosteroids, which is not a favorable option due to their short- and long-term adverse effects. Since it is theorized that the pathophysiology of IRP may possess autoimmune sequelae, the use of immunotherapy for the treatment of IRP has emerged...
January 12, 2017: Pharmacotherapy
https://www.readbyqxmd.com/read/28074640/evaluation-of-pharmacokinetic-interactions-between-lesinurad-a-new-selective-urate-reabsorption-inhibitor-and-commonly-used-drugs-for-gout-treatment
#3
Zancong Shen, Kathy Tieu, David Wilson, Gail Bucci, Michael Gillen, Caroline Lee, Bradley Kerr
Lesinurad is a novel selective uric acid reabsorption inhibitor approved for treatment of hyperuricemia associated with gout in combination with xanthine oxidase inhibitors (XOIs). Open-label pharmacokinetic studies were performed in volunteers or subjects with hyperuricemia (serum uric acid ≥ 8 mg/dL) to investigate interactions of lesinurad (with and without concurrent XOIs) with colchicine and 2 nonsteroidal anti-inflammatory drugs: naproxen and indomethacin. Colchicine studies included consecutive 7-day treatment periods of (1) allopurinol 300 mg, allopurinol 300 mg plus lesinurad 400 or 600 mg, and continued lesinurad 400 or 600 mg; or (2) febuxostat 40 or 80 mg, febuxostat 40 or 80 mg plus lesinurad 400 mg, and continued febuxostat 40 or 80 mg plus lesinurad 600 mg...
January 11, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28065770/risk-of-colchicine-associated-myopathy-in-gout-influence-of-concomitant-use-of-statin
#4
Oh Chan Kwon, Seokchan Hong, Byeongzu Ghang, Yong-Gil Kim, Chang-Keun Lee, Bin Yoo
OBJECTIVE: To investigate the risk of myopathy when statins are coadministered with colchicine in patients with gout. METHODS: In gout patients who received colchicine with or without statin, clinical data collected included medications and history of hypertension, chronic kidney disease, and liver cirrhosis. Myopathy was defined as the presence of muscle symptoms with elevated creatinine phosphokinase and/or myoglobin. Multivariate analysis was performed to identify risk factors for myopathy...
January 5, 2017: American Journal of Medicine
https://www.readbyqxmd.com/read/28065581/nitric-oxide-synthase-inhibitor-aminoguanidine-reduces-intracerebroventricular-colchicine-induced-neurodegeneration-memory-impairments-and-changes-of-systemic-immune-responses-in-rats
#5
Susmita Sil, Tusharkanti Ghosh, Rupsa Ghosh, Pritha Gupta
Intracerebroventricular (i.c.v.) injection of colchicine induces neurodegeneration, memory impairments and changes of some systemic immune responses in rats. Though the role of cox 2 in these colchicine induced changes have been evaluated, the influence of nitric oxide synthase (NOS) remains to be studied. The present study was designed to assess the role of NOS on the i.c.v. colchicine induced neurodegeneration, memory impairments and changes of some systemic immune responses by inhibiting its activity with aminoguanidine...
December 13, 2016: Journal of Neuroimmunology
https://www.readbyqxmd.com/read/28065445/colin-trial-value-of-colchicine-in-the-treatment-of-patients-with-acute-myocardial-infarction-and-inflammatory-response
#6
Mariama Akodad, Benoît Lattuca, Nicolas Nagot, Vera Georgescu, Mathilde Buisson, Jean-Paul Cristol, Florence Leclercq, Jean-Christophe Macia, Richard Gervasoni, Thien-Tri Cung, Stéphane Cade, Frédéric Cransac, Jessica Labour, Anne-Marie Dupuy, François Roubille
BACKGROUND: Inflammation is involved during acute myocardial infarction, and could be an interesting target to prevent ischaemia-reperfusion injuries. Colchicine, known for its pleiotropic anti-inflammatory effects, could decrease systemic inflammation in this context. AIMS: To evaluate the impact of colchicine on inflammation in patients admitted for ST-segment elevation myocardial infarction (STEMI). METHODS: All patients admitted for STEMI with one of the main coronary arteries occluded, and successfully treated with percutaneous coronary intervention, were included consecutively...
January 3, 2017: Archives of Cardiovascular Diseases
https://www.readbyqxmd.com/read/28063128/improved-production-of-doubled-haploids-of-winter-and-spring-triticale-hybrids-via-combination-of-colchicine-treatments-on-anthers-and-regenerated-plants
#7
Aurelia Ślusarkiewicz-Jarzina, Hanna Pudelska, Jolanta Woźna, Tomasz Pniewski
Double haploids (DH), obtained during androgenesis in vitro or by genome diploidisation in regenerated haploids, are one type of basic materials used in triticale breeding programmes. The aim of this study was to improve DH production by a combination of colchicine treatment methods on a sample of five winter and five spring triticale hybrids. Colchicine was applied in vitro either in the C17 medium to induce embryo-like structures (ELS) or in the 190-2 medium for green plant (GP) development. Regenerants which remained haploid were immersed in a colchicine solution either when placed on the medium prior to transferring to soil or when growing in pots, followed by the application or absence of cooling...
January 6, 2017: Journal of Applied Genetics
https://www.readbyqxmd.com/read/28056740/novel-colchicine-derivatives-and-their-anti-cancer-activity
#8
Lorelei Johnson, Ing Swie Goping, Aja Rieger, Jonathan Y Mane, Torin Huzil, Asok Banerjee, Richard Luduena, Bashar Hassani, Philip Winter, Jack A Tuszynski
In this paper we provide an overview of the status of various colchicine derivatives in pre-clinical development with special focus on their anti-cancer activity. We discuss several groups of compounds that have been designed to differentially bind with specific affinities for tubulin β isotypes, especially in regard to βIII, which is commonly over-expressed in cancer. Computational prediction, protein-based and cell-based assays are summarized as well as some animal tests conducted on these compounds. It is concluded that an untapped potential exists for exploiting the colchicine scaffold as a pharmacophore with the possibility of increasing its affinity for tubulin isotypes over-expressed in cancer and decreasing it for normal cells thereby widening the therapeutic window...
January 4, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28056738/microtubule-targeting-agents-as-cancer-chemotherapeutics-an-overview-of-molecular-hybrids-as-stabilising-and-destabilising-agents
#9
Anjana Devi Tangutur, Dinesh Kumar, Kommalapati Vamsi Krishna, Srinivas Kantevari, Anjana Devi Tangutur, Dinesh Kumar, Kommalapati Vamsi Krishna, Srinivas Kantevari
Microtubules form crucial dynamic structural cellular components of the cell and are composed of the alpha beta tubulin heterodimers. Microtubules are involved in a wide variety of functions in the cell such as attribution to cell shape, motility, intracellular trafficking and mitotic spindle formation. Owing to these reasons, tubulin and microtubules have gained significant interest as important targets for cancer therapy. A review of the existing microtubule targeting drugs specifies that these agents can be categorised into two of the major categories: Microtubule stabilising agents such as paclitaxel, docetaxel, epothilones, and discodermolide which bind to the tubulin polymer and stabilize the microtubules, microtubule destabilising agents such as vinca alkaloids, colchicine and combretastatins which bind to tubulin dimers and cause destabilisation...
January 4, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28056737/elucidation-of-the-tubulin-targeted-mechanism-of-action-of-9-3-pyridyl-noscapine
#10
Swagat Pradhan, Tejashree Mahaddalkar, Sinjan Choudhary, Naresh Manhcukonda, Praveen Reddy Nagireddy, Srinivas Kantevari, Manu Lopus
We have recently reported the synthesis and antiproliferative potential of a series of biaryl type α-noscapine congeners. Among them, 9-(3-pyridyl) noscapine 3f (9-PyNos, henceforth), which was synthesized by adding pyridine unit to the tetrahydroisoquinoline part of natural α-noscapine core, was found to be the most effective one to inhibit proliferation of a variety of cancer cell lines. However, details of its interactions with its cellular target, tubulin, remain poorly understood. In this report, we examined the nature of interactions of 9-PyNos with tubulin based on the methodologies of spectrofluorimetry, circular dichroism, and turbidimetry techniques...
4, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28054351/hidradenitis-suppurativa-treated-with-tetracycline-in-combination-with-colchicine-a-prospective-series-of-20-patients
#11
Kalliopi Armyra, Anargyros Kouris, Vasiliki Markantoni, Andreas Katsambas, George Kontochristopoulos
BACKGROUND: Hidradenitis suppurativa (HS) is a chronic inflammatory skin disorder of the follicular epithelium. OBJECTIVES: The objective of the present study was to evaluate the effectiveness of the combination of tetracycline with colchicine in the treatment of HS. METHODS: Twenty patients (10 women and 10 men) with HS were included in an open, prospective, pilot study. All patients were treated with 100 mg minocycline administered orally once per day in combination with 0...
January 4, 2017: International Journal of Dermatology
https://www.readbyqxmd.com/read/28049514/colchicine-triggered-severe-rhabdomyolysis-after-long-term-low-dose-simvastatin-therapy-a-case-report
#12
Clara Frydrychowicz, Bastian Pasieka, Matthias Pierer, Wolf Mueller, Sirak Petros, Lorenz Weidhase
BACKGROUND: Rhabdomyolysis is a widely recognized yet rare complication in statin use. Rhabdomyolysis might be triggered by the prescription of high doses of statins or by statin accumulation due to interactions with concomitant medication. Muscle cell destruction as evidenced by myoglobin elevation can induce potentially life-threatening acute renal failure. CASE PRESENTATION: We report a case of a 70-year-old obese white man with sudden onset of severe rhabdomyolysis with consecutive renal failure...
January 4, 2017: Journal of Medical Case Reports
https://www.readbyqxmd.com/read/28045256/n-heterocyclic-4-phenylpiperazin-1-yl-methanones-derived-from-phenoxazine-and-phenothiazine-as-highly-potent-inhibitors-of-tubulin-polymerization
#13
Helge Prinz, Ann-Kathrin Ridder, Kirsten Vogel, Konrad J Böhm, Igor Ivanov, Jahan B Ghasemi, Elham Aghaee, Klaus Müller
We report here a series of 27 10-(4-phenylpiperazin-1-yl)methanones derived from tricyclic heterocycles which were screened for effects on tumor cell growth, inhibition of tubulin polymerization, and induction of cell cycle arrest. Several analogues, among them the 10-(4-(3-methoxyphenyl)piperazine-1-carbonyl)-10H-phenoxazine-3-carbonitrile (16o), showed excellent antiproliferative properties, with low nanomolar GI50 values (16o, mean GI50 of 3.3 nM) against a large number (93) of cancer cell lines. Fifteen compounds potently inhibited tubulin polymerization...
January 13, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28042127/longterm-beneficial-effect-of-canakinumab-in-colchicine-resistant-familial-mediterranean-fever
#14
Katerina Laskari, Panagiota Boura, George N Dalekos, Alexandros Garyfallos, Dimitrios Karokis, Dimitrios Pikazis, Loukas Settas, Grigoris Skarantavos, Elena Tsitsami, Petros P Sfikakis
OBJECTIVE: To assess the efficacy and safety of the interleukin-1β (IL-1β) inhibitor canakinumab in all adolescent and adult patients with familial Mediterranean fever (FMF) identified from the Greek National Registry for off-label drug use between 2010 and 2015. METHODS: In this retrospective longitudinal outcome study, clinical and laboratory data were collected from 14 patients (7 men) aged median 38.5 years (range 13-70), with median disease duration of 14 years, and active FMF despite colchicine (n = 9) or both colchicine and anakinra (n = 5)...
January 2017: Journal of Rheumatology
https://www.readbyqxmd.com/read/28040706/familial-mediterranean-fever-associated-diseases-in-children
#15
Z Birsin Özçakar, Nilgün Çakar, Nermin Uncu, Banu Acar Çelikel, Fatoş Yalçınkaya
BACKGROUND: MEditerranean FeVer (MEFV) gene encodes for the pyrin protein and a mutated pyrin is associated with a prolonged or augmented inflammation. Hence, various diseases were reported to be associated with familial Mediterranean fever (FMF) or carriers of MEFV mutations. However, systematic evaluation of all associated diseases in children with FMF has not been done previously. AIM: The aim of this study was to investigate the frequency and type of FMF-associated diseases in children...
December 30, 2016: QJM: Monthly Journal of the Association of Physicians
https://www.readbyqxmd.com/read/28040245/the-rising-prevalence-and-incidence-of-gout-in-british-columbia-canada-population-based-trends-from-2000-to-2012
#16
Sharan K Rai, J Antonio Aviña-Zubieta, Natalie McCormick, Mary A De Vera, Kam Shojania, Eric C Sayre, Hyon K Choi
OBJECTIVES: Gout is increasingly recognized as the most common form of inflammatory arthritis worldwide; however, no Canadian data on the disease burden of gout are available. We estimated the prevalence, incidence, prescription patterns, and comorbidity burden of gout in an entire Canadian province [British Columbia (BC)] over the last decade. METHODS: We utilized PopulationData BC, a province-wide database, to estimate temporal trends in the prevalence and incidence of gout from 2000 to 2012, as well as according to age category...
August 17, 2016: Seminars in Arthritis and Rheumatism
https://www.readbyqxmd.com/read/28038323/synthesis-and-biological-evaluation-of-curcumin-inspired-indole-analogues-as-tubulin-polymerization-inhibitors
#17
P V Sri Ramya, Srinivas Angapelly, Lalita Guntuku, Chander Singh Digwal, Bathini Nagendra Babu, V G M Naidu, Ahmed Kamal
In our endeavour towards the development of potent cytotoxic agents, a series of some new curcumin inspired indole analogues, in which indole and phenyl moieties are linked on either sides of 1,5-diaryl-1,4-pentadien-3-one system have been synthesized and characterized by spectral data. All the newly synthesized analogues were tested for their cytotoxic potential against a panel of eight cancer cell lines namely, lung (A549), breast (MDA-MB-231, BT549 and 4T1), prostate (PC-3, DU145), gastric (HGC-27) and cervical (HeLa)...
December 23, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28035796/structural-insights-into-the-inhibition-of-tubulin-by-the-antitumor-agent-4%C3%AE-s-1-2-4-triazole-3-yl-podophyllotoxin
#18
Wei Zhao, Chen Zhou, Ze-Yuan Guan, Ping Yin, Fusheng Chen, Ya-Jie Tang
The colchicine domain was widely recognized as the binding site of the microtubule depolymerization agents for anticancer drug design. Almost all of drugs targeting the colchicine domain have been confirmed to bind to the tubulin β-subunit. Here, we studied a crystal structure (2.3 Å) of the complex between tubulin and 4β-S-(1, 2, 4-triazole-3-yl)-podophyllotoxin (Compound 1S) with superior antitumor activity, which was designed based on the colchicine domain and synthesized in our previous work. A distinct binding model of the colchicine domain was found in the complexes of tubulin-compound 1S...
December 30, 2016: ACS Chemical Biology
https://www.readbyqxmd.com/read/28034647/synthesis-and-biological-evaluation-of-cis-restricted-triazole-tetrazole-mimics-of-combretastatin-benzothiazole-hybrids-as-tubulin-polymerization-inhibitors-and-apoptosis-inducers
#19
A V Subba Rao, Konderu Swapna, Siddiq Pasha Shaik, V Lakshma Nayak, T Srinivasa Reddy, Satish Sunkari, Thokhir Basha Shaik, Chandrakant Bagul, Ahmed Kamal
A series of colchicine site binding tubulin inhibitors were synthesized by the modification of the combretastatin pharmacophore. The ring B was replaced by the pharmacologically relevant benzothiazole scaffolds, and the cis configuration of the olefinic bond was restricted by the incorporation of a triazole and tetrazole rings which is envisaged by the structural resemblance to a tubulin inhibitor like combretastatin (CA-4). These compounds were evaluated for their antiproliferative activity on selected cancer cell lines and an insight in the structure activity relationship was developed...
December 9, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28032450/synthesis-molecular-docking-and-biological-evaluation-of-1-phenylsulfonyl-2-1-methylindol-3-yl-benzimidazole-derivatives-as-novel-potential-tubulin-assembling-inhibitors
#20
Yan-Ting Wang, Xun-Chao Cai, Tian-Qi Shi, Ya-Liang Zhang, Zhong-Chang Wang, Chang-Hong Liu, Hai-Liang Zhu
A series of new 1-phenylsulfonyl-2-(1-methylindol-3-yl)-benzimidazole derivatives were designed, synthesized and evaluated as potential inhibitors of tubulin polymerization and anthropic cancer cell lines. Among them, compound 33 displayed the most potent tubulin polymerization inhibitory activity in vitro (IC50 = 1.41 μM) and strong antiproliferative activities against A549, Hela, HepG2 and MCF-7 cell lines in vitro with GI50 value of 1.6, 2.7, 2.9 and 4.3 μM, respectively comparable with the positive control colchicine (GI50 value of 4...
December 29, 2016: Chemical Biology & Drug Design
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