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https://www.readbyqxmd.com/read/28523104/3-aroyl-1-4-diarylpyrroles-inhibit-chronic-myeloid-leukemia-cell-growth-through-an-interaction-with-tubulin
#1
Giuseppe La Regina, Ruoli Bai, Antonio Coluccia, Valeria Famiglini, Sara Passacantilli, Valentina Naccarato, Giorgio Ortar, Carmela Mazzoccoli, Vitalba Ruggieri, Francesca Agriesti, Claudia Piccoli, Tiziana Tataranni, Marianna Nalli, Andrea Brancale, Stefania Vultaggio, Ciro Mercurio, Mario Varasi, Concetta Saponaro, Sara Sergio, Michele Maffia, Addolorata Maria Luce Coluccia, Ernest Hamel, Romano Silvestri
We designed 3-aroyl-1,4-diarylpyrrole (ARDAP) derivatives as potential anticancer agents having different substituents at the 1- or 4-phenyl ring. ARDAP compounds exhibited potent inhibition of tubulin polymerization, binding of colchicine to tubulin, and cancer cell growth. ARDAP derivative 10 inhibited the proliferation of BCR/ABL-expressing KU812 and LAMA84 cells from chronic myeloid leukemia (CML) patients in blast crisis and of hematopoietic cells ectopically expressing the imatinib mesylate (IM)-sensitive KBM5-WT or its IM-resistant KBM5-T315I mutation...
May 11, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28522413/microglia-support-atf3-positive-neurons-following-hypoglossal-nerve-axotomy
#2
Tatsuhide Tanaka, Koichi Murakami, Yoshio Bando, Taichi Nomura, Ayami Isonishi, Shoko Morita-Takemura, Kouko Tatsumi, Akio Wanaka, Shigetaka Yoshida
Microglia are essential in developmental processes and maintenance of neuronal homeostasis. Experimental axotomy of motor neurons results in neurodegeneration, and microglia in motor nuclei become activated and migrate towards injured neurons. However, whether these activated microglia are protective or destructive to neurons remains controversial. In the present study, we transected the hypoglossal nerve in BALB/c mice, causing activating transcription factor 3 (ATF3) and growth associated protein 43 (GAP43) induction, and partial neuronal death...
May 15, 2017: Neurochemistry International
https://www.readbyqxmd.com/read/28517369/treatment-of-primary-biliary-cholangitis-non-responders-a-systematic-review
#3
Duminda Suraweera, Harman Rahal, Melissa Jimenez, Matthew Viramontes, Gina Choi, Sammy Saab
BACKGROUND: Primary biliary cholangitis (PBC), formerly known as primary biliary cirrhosis, is a chronic cholestatic liver disease characterized by an immune mediated destruction of intrahepatic bile ducts. Ursodeoxycholic acid (UDCA) has been the primary medication for the treatment of PBC, resulting in improved liver tests, resolution of symptoms and increased transplant free survival. However, not all patients respond to UDCA. The aim of this systematic review is to provide an evidence based assessment of the medications that have been studied in patients who are refractory to UDCA...
May 18, 2017: Liver International: Official Journal of the International Association for the Study of the Liver
https://www.readbyqxmd.com/read/28513247/use-of-non-biologic-treatments-in-antihistamine-refractory-chronic-urticaria-a-review-of-published-evidence
#4
Jesper Grønlund Holm, Ilya Ivyanskiy, Simon Francis Thomsen
BACKGROUND: Knowledge of effectiveness and safety of the non-biologic, non-antihistamine treatments used for chronic urticaria is important as in some cases the principal guideline-recommended drug; omalizumab, has limited effect, side effects, or is too expensive or unavailable. Herein we systematically review the evidence for the use of the non-biologic treatments in antihistamine-refractory chronic urticaria. METHODS: We performed a systematic review of the literature using PubMed and Webofscience and identified studies that reported use of one or more of the non-biological, non-antihistamine treatment options for chronic urticaria...
May 17, 2017: Journal of Dermatological Treatment
https://www.readbyqxmd.com/read/28512995/alpha-1-antitrypsin-deficiency-related-panniculitis-two-cases-with-diverse-clinical-courses
#5
E R Storan, S M O' Gorman, P Hawkins, L Aalto, A Murphy, T Markham
Alpha-1-antitrypsin deficiency (AATD)-related panniculitis is an extremely rare and underdiagnosed entity, and there is a paucity of data on its treatment. We report two cases of AATD-related panniculitis. The first was a 24-year-old woman with known AATD who presented with painful leg ulcers refractory to treatment with corticosteroids and colchicine. She had a good response to α1-antitrypsin infusions but required dose adjustment due to flares in disease activity. The second case was a 38-year-old woman who presented with painful nodules on the legs refractory to corticosteroid therapy...
May 17, 2017: Clinical and Experimental Dermatology
https://www.readbyqxmd.com/read/28510185/morphological-physiological-cytological-and-phytochemical-studies-in-diploid-and-colchicine-induced-tetraploid-plants-of-fagopyrum-tataricum-l-gaertn
#6
Lin-Jiao Wang, Mao-Yin Sheng, Pei-Cai Wen, Jia-Ying Du
BACKGROUND: Tartary buckwheat are very popular as an important functional food material and its cultivation is very widespread in our whole world, but there obviously lack works in the researches of genetic breeding for agricultural and medicinal utilization. The aim of this study is to obtain good germplasm resources for agricultural and medicinal use of tartary buckwheat (Fagopyrum tataricum) by inducing the tetraploid plants. RESULTS: Four cultivars of F. tataricum, that is, Qianwei 2#, Jinku 2#, Chuanqiao 1#, and Liuqiao 1# were selected to experiment...
December 2017: Botanical Studies (Taipei, Taiwan)
https://www.readbyqxmd.com/read/28502672/dta0100-dual-topoisomerase-ii-and-microtubule-inhibitor-evades-paclitaxel-resistance-in-p-glycoprotein-overexpressing-cancer-cells
#7
Ana Podolski-Renić, Jasna Banković, Jelena Dinić, Carla Ríos-Luci, Miguel X Fernandes, Nuria Ortega, Nataša Kovačević-Grujičić, Víctor S Martín, José M Padrón, Milica Pešić
The efficacy of microtubule targeting agents in cancer treatment has been compromised by the development of drug resistance that may involve both, P-glycoprotein overexpression and the changes in β-tubulin isoforms' expression. The anti-Topoisomerase II activity of methyl 4-((E)-2-(methoxycarbonyl)vinyloxy)oct-2-ynoate (DTA0100) was recently reported. Herein, we further evaluated this propargylic enol ether derivative and found that it exerts inhibitory effect on tubulin polymerization by binding to colchicine binding site...
May 11, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28497352/monogenic-periodic-fever-syndromes-treatment-options-for-the-pediatric-patient
#8
REVIEW
Seza Ozen, Selcan Demir
Autoinflammatory diseases are disorders of the innate immune system characterized by uncontrolled inflammation. The most commonly encountered autoinflammatory diseases are the hereditary periodic fever syndromes, which present with fever and other features of the skin, serosal membranes, and musculoskeletal system. The main inherited (monogenic) periodic fever syndromes are familial Mediterranean fever (FMF), cryopyrin-associated periodic syndrome (CAPS), tumor necrosis factor receptor-associated periodic syndrome (TRAPS), and hyperimmunoglobulin D syndrome (HIDS)/mevalonate kinase deficiency (MKD)...
May 11, 2017: Paediatric Drugs
https://www.readbyqxmd.com/read/28492007/colchicine-may-assist-in-reducing-granulation-tissue-in-junctional-epidermolysis-bullosa
#9
Minhee Kim, Swaranjali Jain, Adam G Harris, Dedee F Murrell
Epidermolysis bullosa (EB) is a rare, inherited blistering genodermatosis. Patients with junctional EB (JEB) due to LAMB3 mutations have widespread blisters and erosions of skin, mucosae, and nails, creating significant physical, emotional, and psychosocial burdens. Here we report the use of colchicine for ameliorating hypergranulating wounds in a 41-year-old female with JEB generalized intermediate. Her skin wounds and granulation tissue gradually exacerbated under silicone dressings such that she became profoundly anemic...
June 2016: International Journal of Women's Dermatology
https://www.readbyqxmd.com/read/28487937/colchicine-attenuates-renal-fibrosis-in-a-murine-unilateral-ureteral-obstruction-model
#10
Seiji Itano, Minoru Satoh, Hiroyuki Kadoya, Yuji Sogawa, Atsushi Uchida, Tamaki Sasaki, Naoki Kashihara
The present study aimed to assess the effects of colchicine, a known anti‑inflammatory agent, on renal fibrosis using a murine model of unilateral ureteral obstruction (UUO). Male C57BL/6 mice were divided into two groups, vehicle‑ and colchicine‑treated. Colchicine (0.5 mg/kg/day) was administered by osmotic pump, and the UUO procedure was performed on the left kidney 7 days later. The mice were sacrificed at 14 days following UUO. Colchicine treatment suppressed interstitial fibrosis of the UUO kidneys...
June 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28485997/prophylaxis-of-acute-flares-when-initiating-febuxostat-for-chronic-gouty-arthritis-in-a-real-world-clinical-setting
#11
Jinquan Yu, Qian Qiu, Liuqin Liang, Xiuyan Yang, Hanshi Xu
OBJECTIVE: Flare prophylaxis is recommended during urate-lowering therapy (ULT) despite lack of proven benefit especially when initiating febuxostat. We investigated if colchicine or steroids administration during initiation of febuxostat for chronic gouty arthritis reduces the frequency and/or severity of acute gout flares. METHODS: Patients with confirmed diagnosis of gout starting febuxostat were retrospectively studied. Frequency, severity, and length of flares were analyzed...
May 9, 2017: Modern Rheumatology
https://www.readbyqxmd.com/read/28484934/novel-antimitotic-agents-related-to-tubuloclustin-synthesis-and-biological-evaluation
#12
Olga N Zefirova, Evgeniya V Nurieva, Birgit Wobith, Vladimir V Gogol, Nikolay A Zefirov, Andrei V Ogonkov, Dmitrii V Shishov, Nikolay S Zefirov, Sergei A Kuznetsov
Tubuloclustin [N-(7-adamant-2-yloxy-7-oxoheptanoyl)-N-deacetylcolchicine], a highly cytotoxic anti-tubulin compound is known for its ability to promote microtubule disassembly followed by the formation of tubulin clusters of unique morphology. Three series of antimitotic agents related to tubuloclustin were designed and synthesized in order to enhance the molecular diversity of "tubuloclustin-like" family of compounds. The series of compounds with modified adamantane moiety was highly potent in cytotoxic effect on human lung carcinoma A549 cells (EC50 = 6-400 nM) and was active in affecting the microtubule arrays and induction of strong tubulin clusterization...
May 8, 2017: Molecular Diversity
https://www.readbyqxmd.com/read/28483439/ustekinumab-for-beh%C3%A3-et-s-disease
#13
Adrien Mirouse, Stéphane Barete, Jean-Benoît Monfort, Matthieu Resche-Rigon, Anne-Sophie Bouyer, Cloé Comarmond, Damien Sène, Fanny Domont, Yasmina Ferfar, Patrice Cacoub, David Saadoun
OBJECTIVE: To evaluate the efficacy and safety of ustekinumab in the treatment of oral ulcers (OU) in patients with Behçet's disease (BD). PATIENTS AND METHODS: Prospective study including 14 patients [median age of 39 (34; 41) years, with 71% of men] fulfilling criteria of the International Study Group for BD and with active OU resistant to colchicine. Patients received ustekinumab 90 mg (n = 11) or 45 mg (n = 3) subcutaneously at inclusion, at week 4, and every 12 weeks...
May 5, 2017: Journal of Autoimmunity
https://www.readbyqxmd.com/read/28482392/-three-cases-with-familial-mediterranean-fever-misdiagnosed-as-juvenile-idiopathic-arthritis
#14
J Li, Y Zhang, W Wang, L Q Zhong, H M Song
Objective: To explore the key points of diagnosis and treatment of familial Mediterranean fever(FMF). Method: The clinical data of 3 cases with FMF misdiagnosed as Juvenile idiopathic arthritis(JIA)seen from January 2014 to June 2016 in Peking Union Medical College Hospital were retrospectively collected. The clinical manifestations, gene mutation characteristics, treatment and prognosis were also evaluated. Result: Two cases were male and 1 was female. The mean age of onset was 17 months (3 months to 36 months), while the average age of diagnosis was 6 years and 8 months (24 months to 11 years)...
May 4, 2017: Zhonghua Er Ke za Zhi. Chinese Journal of Pediatrics
https://www.readbyqxmd.com/read/28481234/protective-effects-of-amarogentin-against-carbon-tetrachloride-induced-liver-fibrosis-in-mice
#15
Ya Zhang, Hang Zhao, Hua Li, Wei Cao, Fang Wang, Tian Zhang, Si-Wang Wang
Amarogentin, a secoiridoid glycoside that is mainly extracted from Swertia and Gentiana roots, has been suggested to exhibit many biological effects, including anti-oxidative, anti-tumour, and anti-diabetic activities. The present study was designed to evaluate the protective effects of amarogentin on carbon tetrachloride-induced liver fibrosis in vivo and the underlying mechanism. Fibrosis was induced by subcutaneous injections of 6 mL/kg of 20% carbon tetrachloride (dissolved in olive oil) twice per week for seven weeks...
May 6, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28480402/effect-of-ruanganjiedu-decoction-inhibit-experimental-hepatic-fibrosis-of-rats
#16
Sheng Liu, Xiao-Min Wang, Guo-Wang Yang
BACKGROUND: RuanGanJieDu (RGJD) is a traditional Chinese medicine comprising nine Chinese medicinal herbs. The clinical use of RGJD by us was found that it has a good control effect on hepatic fibrosis (HF) patient. In order to further investigate the Anti-fibrosis mechanism of RGJD, hence this experiment has been carried out. METHODS: After treatment, the general conditions of rats in each group were observed. The liver tissues morphology and HF phases were observed under light microscope...
2017: African Journal of Traditional, Complementary, and Alternative Medicines: AJTCAM
https://www.readbyqxmd.com/read/28468964/luminal-angiotensin-ii-is-internalized-as-a-complex-with-at1r-at2r-heterodimers-to-target-endoplasmic-reticulum-in-llc-pk1-cells
#17
Fernanda M Ferrão, Luiza H D Cardoso, Heather A Drummond, Xiao C Li, Jia L Zhuo, Dayene S Gomes, Lucienne S Lara, Adalberto Vieyra, Jennifer Lowe
Angiotensin II (ANG II) has many biological effects in renal physiology, particularly in Ca(2+) handling in the regulation of fluid and solute reabsorption. It involves the systemic endocrine renin-angiotensin system (RAS), but tissue and intracrine ANG II are also known. We have shown that ANG II induces heterodimerization of its AT1 and AT2 receptors (AT1R and AT2R) to stimulate sarco(endo)plasmic reticulum Ca(2+)-ATPase (SERCA) activity. Thus, we investigated whether ANG II-AT1R/AT2R complex is formed and internalized, and also looked at the intracellular localization of this complex to determine how its effect might be exerted on renal intracrine RAS...
May 3, 2017: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/28462842/design-and-synthesis-of-1-2-3-triazolo-linked-benzo-d-imidazo-2-1-b-thiazole-conjugates-as-tubulin-polymerization-inhibitors
#18
Siddiq Pasha Shaik, M V P S Vishnuvardhan, Faria Sultana, A V Subba Rao, Chandrakant Bagul, Debanjan Bhattacharjee, Jeevak Sopanrao Kapure, Nishant Jain, Ahmed Kamal
1,2,3-Triazolo linked benzo[d]imidazo[2,1-b]thiazole conjugates (5a-v) were designed, synthesized and evaluated for their cytotoxic potency against some human cancer cell lines like DU-145 (prostate), HeLa (cervical), MCF-7 (breast) HepG2 (liver) and A549 (lung). Preliminary results revealed that some of these conjugates like 5f and 5k exhibited significant antiproliferative effect against human breast cancer cells (MCF-7) with IC50 values of 0.60 and 0.78µM respectively. Flow cytometric analysis of the cell cycle demonstrated an increase in the percentage of cells in the G2/M phase which was further authenticated by elevation of cyclin B1 protein levels...
April 12, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28461812/refractory-cutaneous-iga-vasculitis-treated-with-omega-3-fatty-acids
#19
M A Barnadas, M M Díaz Encarnación
BACKGROUND: Omega-3 fatty acids (O3FA) have been used to treat IgA nephropathy (IgAN) but not cutaneous IgA vasculitis (IgAV). CASE REPORT: A 47-year-old female was referred for cutaneous vasculitis. She had a 24-year history of flares of palpable purpura, arthralgia associated with hematuria, and proteinuria. We diagnosed cutaneous IgAV associated with IgAN. We administered prednisone at doses ranging from 10 to 45 mg/day to control the flares. To reduce prednisone exposure, different therapeutic strategies (colchicine, diphenhydramine, hydroxyzine, azathioprine, benzathine penicillin, and mycophenolate mofetil) were applied without success...
September 2016: Case Reports in Dermatology
https://www.readbyqxmd.com/read/28461764/abcg2-polymorphisms-in-gout-insights-into-disease-susceptibility-and-treatment-approaches
#20
REVIEW
M C Cleophas, L A Joosten, L K Stamp, N Dalbeth, O M Woodward, Tony R Merriman
As a result of the association of a common polymorphism (rs2231142, Q141K) in the ATP-binding cassette G2 (ABCG2) transporter with serum urate concentration in a genome-wide association study, it was revealed that ABCG2 is an important uric acid transporter. This review discusses the relevance of ABCG2 polymorphisms in gout, possible etiological mechanisms, and treatment approaches. The 141K ABCG2 urate-increasing variant causes instability in the nucleotide-binding domain, leading to decreased surface expression and function...
2017: Pharmacogenomics and Personalized Medicine
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