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https://www.readbyqxmd.com/read/28211616/design-synthesis-and-biological-evaluation-of-chalcone-containing-shikonin-derivatives-as-inhibitors-of-tubulin-polymerization
#1
Han-Yue Qiu, Fang Wang, Xue Wang, Wen-Xue Sun, Jin-Liang Qi, Yan-Jun Pang, Rong-Wu Yang, Gui-Hua Lu, Xiao-Ming Wang, Yong-Hua Yang
The biological importance of microtubules in mitosis makes them an interesting target for the development of anticancer agents. In this study, a series of novel chalcone-containing shikonin derivatives was designed, synthesized, and evaluated for biological activities. Among them, derivative PMMB-259 [(R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl (E)-2-(4-(3-oxo-3-(3-(trifluoromethoxy)phenyl)prop-1-en-1-yl)phenoxy)acetate] was identified as a potent inhibitor of tubulin polymerization...
February 17, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28207965/is-colchicine-more-effective-to-prevent-pfapa-episodes-in-mefv-variants
#2
Muhammed Gunes, Sukru Cekic, Sara Sebnem Kilic
BACKGROUND: Periodic fever, aphthous stomatitis, pharyngitis and cervical adenitis (PFAPA) syndrome is the most frequent repetitive fever syndrome in childhood. It is characterized with fever episodes lasting for about three to six days, once every three to eight weeks. METHODS: Clinical and laboratory data of patients with PFAPA syndrome between January 2010 and December 2014 followed up at a tertiary pediatric care hospital were reviewed. RESULTS: Four-hundred children (256 male, 144 female), the mean age at diagnosis was 4...
February 16, 2017: Pediatrics International: Official Journal of the Japan Pediatric Society
https://www.readbyqxmd.com/read/28188167/hidradenitis-suppurativa-neutrophilic-dermatoses-and-diverticular-disease-in-a-young-african-american-patient
#3
Kavita Darji, Maulik M Dhandha, Mary Guo
Hidradenitis suppurativa (HS) is a chronic skin disorder of the terminal follicular epithelium of apocrine sweat glands, manifesting as painful and exudative papules, pustules, cysts or nodules. This inflammatory condition often presents with other systemic and cutaneous disorders. We present the case of an African-American man with HS who was also diagnosed with neutrophilic dermatoses and diverticular disease. Neutrophilic dermatosis was identified based on histopathology findings. Our patient underwent multiple surgeries for flaring of his skin condition...
February 10, 2017: BMJ Case Reports
https://www.readbyqxmd.com/read/28185680/recurrent-pericarditis
#4
M Imazio, A Battaglia, L Gaido, F Gaita
Recurrent pericarditis is the most troublesome complication of pericarditis occurring in 15 to 30% of cases. The pathogenesis is often presumed to be immune-mediated although a specific rheumatologic diagnosis is commonly difficult to find. The clinical diagnosis is based on recurrent pericarditis chest pain and additional objective evidence of disease activity (e.g. pericardial rub, ECG changes, pericardial effusion, elevation of markers of inflammation, and/or imaging evidence of pericardial inflammation by CT or cardiac MR)...
February 6, 2017: La Revue de Médecine Interne
https://www.readbyqxmd.com/read/28168063/a-rare-case-of-vancomycin-induced-linear-immunoglobulin-a-bullous-dermatosis
#5
Pinky Jha, Kurtis Swanson, Jeremiah Stromich, Basia M Michalski, Edit Olasz
Linear IgA bullous dermatosis (LABD) is an autoimmune vesiculobullous disease, which is typically idiopathic but can also rarely be caused by medications or infections. Vancomycin is the most common drug associated with LABD. Lesions typically appear 24 hours to 15 days after the first dose of vancomycin. It is best characterized pathologically by subepidermal bulla (blister) formation with linear IgA deposition at the dermoepidermal junction. Here we report an 86-year-old male with a history of left knee osteoarthritis who underwent a left knee arthroplasty and subsequently developed a prosthetic joint infection...
2017: Case Reports in Dermatological Medicine
https://www.readbyqxmd.com/read/28166995/design-synthesis-and-anticancer-properties-of-isocombretaquinolines-as-potent-tubulin-assembly-inhibitors
#6
Ilhem Khelifi, Timothée Naret, Dolor Renko, Abdallah Hamze, Guillaume Bernadat, Jérome Bignon, Christine Lenoir, Joëlle Dubois, Jean-Daniel Brion, Olivier Provot, Mouad Alami
The synthesis and evaluation of a new series of IsoCombretaQuinolines (IsoCoQuines) 2 with a 2-substituted-quinoline in place of the 3,4,5-trimethoxyphenyl ring present in isoCA-4 and CA-4 are described. Most of these compounds displayed a potent cytotoxic activity (IC50 < 10 nM) against a panel of five human cancer cell lines and inhibited tubulin assembly at a micromolar level. The most potent analogue 2b, having a 3-hydroxy-4-methoxyphenyl as B-ring, led to cell cycle arrest in G2/M phase. Docking studies indicate that 2b showed a binding mode comparable to those previously observed with quinazoline analogous (IsoCoQ) and with isoCA-4 at the colchicine binding site of tubulin...
February 15, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28153936/the-3-year-incidence-of-gout-in-elderly-patients-with-ckd
#7
Vivian S Tan, Amit X Garg, Eric McArthur, Ngan N Lam, Manish M Sood, Kyla L Naylor
BACKGROUND AND OBJECTIVES: The risk of gout across CKD stages is not well described. DESIGN, SETTING, PARTICIPANTS, & MEASUREMENTS: We performed a retrospective cohort study using linked health care databases from Ontario, Canada from 2002 to 2010. The primary outcome was the 3-year cumulative incidence of gout, on the basis of diagnostic codes. We presented our results by level of kidney function (eGFR≥90 ml/min per 1.73 m(2), 60-89, 45-59, 30-44, 15-29, and chronic dialysis) and by sex...
February 2, 2017: Clinical Journal of the American Society of Nephrology: CJASN
https://www.readbyqxmd.com/read/28150327/new-3-substituted-2-4-hydroxyanilino-pyridine-derivatives-synthesis-antitumor-activity-and-tubulin-polymerization-inhibition
#8
Salwa Elmeligie, Nadia A Khalil, Eman M Ahmed, Soha H Emam
A series of new pyridine derivatives 4a-c, 5a-d, 6a-d, 7a-f, and 8a-f structurally related to ABT-751 were synthesized and characterized by spectroscopic means and elemental analysis. All the synthesized compounds were tested for their cytotoxic activity in vitro against the HCT-116 and HepG-2 cancer cell lines using the MTT assay. The results showed that compound 8d has higher cytotoxic activity than the reference antimitotic agent colchicine, against both tested cell lines, with IC50  = 0.52 and 1.40 μM, respectively...
February 2, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28143677/tubulin-binding-dibenz-c-e-oxepines-part-2-structural-variation-and-biological-evaluation-as-tumour-vasculature-disrupting-agents
#9
Steven B Rossington, John A Hadfield, Steven D Shnyder, Timothy W Wallace, Kaye J Williams
5,7-Dihydro-3,9,10,11-tetramethoxybenz[c,e]oxepin-4-ol 1, prepared from a dibenzyl ether precursor via Pd-catalysed intramolecular direct arylation, possesses broad-spectrum in vitro cytotoxicity towards various tumour cell lines, and induces vascular shutdown, necrosis and growth delay in tumour xenografts in mice at sub-toxic doses. The biological properties of 1 and related compounds can be attributed to their ability to inhibit microtubule assembly at the micromolar level, by binding reversibly to the same site of the tubulin αβ-heterodimer as colchicine 2 and the allocolchinol, N-acetylcolchinol 4...
January 19, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28132142/protocol-for-producing-synthetic-polyploid-oats
#10
Toshinobu Morikawa
A protocol to produce synthetic oats by introducing alien genetic variations into cultivated oats is proposed based on suitable genetic relationships between Avena species. Furthermore, artificial hybridization procedures between different ploidy species are explained. Amphiploids can be produced by rescuing aborted embryos and treating the F1 hybrids with colchicine to overcome sterility between interspecific plants. Furthermore, I present the cytological methods for observing somatic and meiotic chromosomes in the treated hybrids...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28132140/oat-doubled-haploids-following-maize-pollination
#11
Philip A Davies, Parminder K Sidhu
Doubled haploids (DHs) are an important tool for the accelerated production of new crop varieties. In oat, DHs were first produced by pollinating oat florets with maize pollen. The resultant embryos spontaneously eliminate the maize chromosomes leaving a haploid complement of oat chromosomes. These embryos can be cultured in vitro using the "embryo rescue" technique to produce haploid plants whose chromosome number can be doubled with colchicine to produce homozygous DH oat plants.
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28129738/a-novel-case-of-renal-pathergy-reaction-in-a-beh%C3%A3-et-s-disease-patient-complicated-by-iga-vasculitis
#12
Takaaki Higashihara, Akira Okada, Taiko Kusano, Kazuyoshi Ishigaki, Akira Shimizu, Hideki Takano
BACKGROUND: A pathergy reaction is defined as a hyperreactivity of the skin in response to minimal trauma, which is important in the diagnosis of Behçet's disease (BD). However, a pathergy reaction may not be restricted to the skin, and little is known about whether an invasive medical procedure can induce the reaction. Here we present a pathergy reaction induced by renal biopsy, an invasive procedure. CASE PRESENTATION: A 46-year-old man who was diagnosed with IgA vasculitis (IgAV) at the age of 38 was treated with prednisolone and mizoribine...
January 28, 2017: BMC Nephrology
https://www.readbyqxmd.com/read/28120704/qsar-modeling-of-the-arylthioindole-class-of-colchicine-polymerization-inhibitors-as-anticancer-agents
#13
Elnaz Habibpour, Shahin Ahmadi
BACKGROUND: The health and life of humans have been seriously threatened by cancer for a long period and cancer has become the leading disease-related cause of deaths of human population. Natural products such as colchicine and vinblastine inhibit microtubule assembly by preventing tubulin polymerization. GA-MLR is a powerful search technique based on the evolution of biological systems for QSAR modeling. In this paper, we studied QSAR modeling of some arylthioindole class of colchicine polymerization inhibitors as anticancer agents using GA-MLR and stepwise-MLR...
January 23, 2017: Current Computer-aided Drug Design
https://www.readbyqxmd.com/read/28117204/a-novel-piperazine-linked-%C3%AE-amino-alcohols-bearing-a-benzosuberone-scaffolds-as-anti-proliferative-agents
#14
Sowmya Vanguru, Lavanya Jilla, Yasodakrishna Sajja, Rajashaker Bantu, Lingaiah Nagarapu, Jagadeesh Babu Nanubolu, Bala Bhaskar, Nishant Jain, Sreekanth Sivan, Vijjulatha Manga
A new series of 1-((9-chloro-2,3-dimethyl-6,7-dihydro-5H-benzo[7]annulen-8-yl)methoxy)-3-(4-phenylpiperzin-1-yl) propan-2-ols (6a-k) have been designed, synthesized and their structures were established by spectroscopic data (FT-IR, (1)H NMR, (13)C NMR, HRMS) and further confirmed by X-ray analysis. The newly synthesized compounds 6a-k were evaluated for their in vitro anti-proliferative activity against four cancer cell lines such as HeLa (cervical), MDA-MB-231 (breast), A549 (lung) and MIAPACA (pancreatic)...
January 13, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28114299/matrilineal-a-sperm-specific-phospholipase-triggers-maize-haploid-induction
#15
Timothy Kelliher, Dakota Starr, Lee Richbourg, Satya Chintamanani, Brent Delzer, Michael L Nuccio, Julie Green, Zhongying Chen, Jamie McCuiston, Wenling Wang, Tara Liebler, Paul Bullock, Barry Martin
Sexual reproduction in flowering plants involves double fertilization, the union of two sperm from pollen with two sex cells in the female embryo sac. Modern plant breeders increasingly seek to circumvent this process to produce doubled haploid individuals, which derive from the chromosome-doubled cells of the haploid gametophyte. Doubled haploid production fixes recombinant haploid genomes in inbred lines, shaving years off the breeding process. Costly, genotype-dependent tissue culture methods are used in many crops, while seed-based in vivo doubled haploid systems are rare in nature and difficult to manage in breeding programmes...
January 23, 2017: Nature
https://www.readbyqxmd.com/read/28108907/peripapillary-retinal-nerve-fiber-layer-and-ganglion-cell-inner-plexiform-layer-thickness-in-adult-onset-familial-mediterranean-fever
#16
Sait Alim, Mehmet Esen, Ayşe Kevser Demir, Selim Demir, Hüseyin Ortak, Alper Güneş, Tufan Alatli, Helin Deniz Demir
OBJECTIVE: The purpose of the present study was to evaluate the thickness of the peripapillary retinal nerve fiber layer (RNFL) and retinal ganglion cell-inner plexiform layer (GCIPL) in adult-onset familial Mediterranean fever (FMF). METHODS: Forty two adult-onset FMF patients and forty two healthy controls were included in the present study. Detailed ocular examination was performed, and then the thickness of the peripapillary RNFL and GCIPL was measured by Spectral domain optical coherence tomography...
January 21, 2017: International Ophthalmology
https://www.readbyqxmd.com/read/28105271/biological-evaluation-in-vitro-and-in-silico-of-azetidin-2-one-derivatives-as-potential-anticancer-agents
#17
Fabián E Olazaran, Gildardo Rivera, Alondra M Pérez-Vázquez, Cynthia M Morales-Reyes, Aldo Segura-Cabrera, Isaías Balderas-Rentería
Potential anticancer activity of 16 azetidin-2-one derivatives was evaluated showing that compound 6 [N-(p-methoxy-phenyl)-2-(p-methyl-phenyl)-3-phenoxy-azetidin-2-one] presented cytotoxic activity in SiHa cells and B16F10 cells. The caspase-3 assay in B16F10 cells displayed that azetidin-2-one derivatives induce apoptosis. Microarray and molecular analysis showed that compound 6 was involved on specific gene overexpression of cytoskeleton regulation and apoptosis due to the inhibition of some cell cycle genes...
January 12, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28101833/gout-treatment-survey-of-brazilian-rheumatology-residents
#18
REVIEW
Rodrigo Balbino Chaves Amorim, Ana Beatriz Vargas-Santos, Leticia Rocha Pereira, Evandro Silva Freire Coutinho, Geraldo da Rocha Castelar-Pinheiro
To assess the current practices in gout management among Brazilian rheumatology residents. We performed a cross-sectional online survey among all the rheumatology residents and those rheumatologists who had just completed their training (post-residency (PR)) regarding their approach to gout management. Results were compared with the 2012 American College of Rheumatology (ACR) gout guidelines and with the responses of a previous survey with a representative sample of practicing Brazilian rheumatologists (RHE)...
January 19, 2017: Clinical Rheumatology
https://www.readbyqxmd.com/read/28097903/treatment-of-familial-mediterranean-fever-with-anakinra-in-patients-unresponsive-to-colchicine
#19
A-C Pecher, A Igney-Oertel, L Kanz, J Henes
No abstract text is available yet for this article.
January 18, 2017: Scandinavian Journal of Rheumatology
https://www.readbyqxmd.com/read/28089200/limitations-of-the-current-standards-of-care-for-treating-gout-and-crystal-deposition-in-the-primary-care-setting-a-review
#20
Robert T Keenan
PURPOSE: This article outlines several important issues regarding the management of patients with gout. The topics discussed include best practices for gout based on the most current guidelines, opportunities for improving gout management, and current and emerging therapies for gout. METHODS: [PubMed and Google Scholar databases] were search for all articles and trials published before 2016, using the key terms [hyperuricemia, gout, tophi, joint erosion, joint damage, treatment guidelines, American College of Rheumatology (ACR), European League Against Rheumatism (EULAR), flare, comorbidity, epidemiology, adherence, serum uric acid (sUA), monosodium urate (MSU), <6 mg/dL, MSU crystal formation, as well as individual drug names and classes of treatments of interest (allopurinol, febuxostat, colchicine, non-steroidal anti-inflammatories (NSAIDs)]...
January 11, 2017: Clinical Therapeutics
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