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Malihe Hassanzadeh, Kowsar Bagherzadeh, Massoud Amanlou
Nowadays the ability to prediction of complex behavior rationally based on the computational approaches has been a successful technique in drug discovery. In the present study interactions of a new series of hybrids, which were made by linking colchicine as a tubulin inhibitor and suberoylanilide hydroxamic acid (SAHA) as a HDAC inhibitor, with HDAC8 and HDAC1 were investigated and compared. This research has been facilitated by the availability of experimental information besides employing docking methodology as well as classical molecular dynamics simulations and binding free energy calculation were performed...
October 7, 2016: Journal of Molecular Graphics & Modelling
Yi-Chia Su, Chih-Chien Wu
A 54-year-old woman presented at the emergency department after experiencing lower limb weakness and bilateral ankle pain for 2 days. She had a history of type 2 diabetes mellitus, diabetes mellitus nephropathy with chronic kidney disease, and chronic gouty arthritis. She had received 0.6 mg colchicine orally once or twice daily for 8 months. Four days prior to her emergency department visit, she was discharged from our nephrology ward, where she had been admitted because of a urinary tract infection. During hospitalization, she was treated with intravenous cefazolin for 7 days...
December 2015: Drug Saf Case Rep
Salwa Elmeligie, Azza T Taher, Nadia A Khalil, Ahmed H El-Said
Novel series of 1,3,4-trisubstituted azetidin-2-one derivatives 8a-p were synthesized and proposed as cytotoxic agents acting via inhibition of tubulin at the colchicine binding site. The design of the target compounds was based upon modification in the structure of the vascular targeting agent combretastatin A-4 (CA-4). The cis double bond linker in CA-4 was replaced with the azetidin-2-one ring aiming to prevent the cis/trans isomerization that suppresses the activity of CA-4, thereby enhancing its antiproliferative activity...
October 17, 2016: Archives of Pharmacal Research
Ri Gao, Haibin Wang, Bin Dong, Xiaodong Yang, Sumei Chen, Jiafu Jiang, Zhaohe Zhang, Chen Liu, Nan Zhao, Fadi Chen
Autopolyploidy is widespread in higher plants and plays an important role in the process of evolution. The present study successfully induced autotetraploidys from Chrysanthemum lavandulifolium by colchicine. The plant morphology, genomic, transcriptomic, and epigenetic changes between tetraploid and diploid plants were investigated. Ligulate flower, tubular flower and leaves of tetraploid plants were greater than those of the diploid plants. Compared with diploid plants, the genome changed as a consequence of polyploidization in tetraploid plants, namely, 1...
October 9, 2016: International Journal of Molecular Sciences
Kenji Takeshita, Hiroaki I Ogawa, Toshinari Maeda
BACKGROUND: Carcinogens are known to cause swelling of the mammalian cell nucleus. However, the mechanism of the swelling and its toxicological significance have not been fully elucidated. Since nuclear swelling (NS hereafter) has been frequently observed in chromosomal aberration (CA hereafter) tests (in vitro), the relationship between NS and CAs was investigated in this study. RESULTS: In a short-term CA test using the fibroblast CHL cell line, the appearance of NS increased in a dose-dependent manner after exposure to six types of clastogens (mitomycin C, methyl methane sulfonate, 1-methyl-3-nitro-1-nitrosoguanidine, benzo[a]pyrene, cyclophosphamide monohydrate, and 9,10-dimethyl-2-benzanthracene), and a strong correlation was found between NS (%) and CAs (%) at each dosage...
2016: Genes and Environment: the Official Journal of the Japanese Environmental Mutagen Society
Kei Tsutsui, Masahiro Otoh, Kodama Sakurai, Nami Suzuki-Hashido, Takashi Hayakawa, Takumi Misaka, Yoshiro Ishimaru, Filippo Aureli, Amanda D Melin, Shoji Kawamura, Hiroo Imai
BACKGROUND: New World monkeys (NWMs) are unique in that they exhibit remarkable interspecific variation in color vision and feeding behavior, making them an excellent model for studying sensory ecology. However, it is largely unknown whether non-visual senses co-vary with feeding ecology, especially gustation, which is expected to be indispensable in food selection. Bitter taste, which is mediated by bitter taste receptors (TAS2Rs) in the tongue, helps organisms avoid ingesting potentially toxic substances in food...
October 12, 2016: BMC Evolutionary Biology
Yasir Mehmood, Humayun Riaz, Hammad Yousaf, Syed Atif Raza, Rana Khalid Mahmood, Zia Mohy-Ud-Din Khan, Noviara Saleem
Present investigation concern with combination of two drugs for the treatment of gout. One of these drug (naproxen sodium) is pain killer which is sustain their action within the body for 12 hours and the other drug (colchicine) is anti-gout, which release as conventional dosage. After oral administration naproxen will act as sustain release dosage and increase patient compliance about six batches of tablet were developed and evaluate .For the sustain release action polymers Methocel K4M and HPMCK15were used...
September 2016: Pakistan Journal of Pharmaceutical Sciences
B Lakshmi Divya, P Narasimha Rao
SAPHO syndrome (synovitis, acne, pustulosis, hyperostosis, osteitis), a rare inflammatory disorder, is an association of distinct skin disorders with pustules with osteoarticular inflammation. Its etiology remains unclear, and various treatment regimens frequently fail to control the disease. An 18-year-old male patient presented to the outpatient department with severe nodulocystic acne on the face with pain at both the wrists and lower back associated with high-grade fever and chills. On physical examination, he had severe tenderness at both wrist joints and lower back, along with swelling of right wrist...
September 2016: Indian Dermatology Online Journal
Hisako Karube, Koju Kamoi, Kyoko Ohno-Matsui
BACKGROUND: Ocular symptoms in Behçet's disease (BD) begin mostly before 30 years of age according to international surveys, and BD activity may decrease with age. Information regarding the treatment of ocular symptoms in elderly BD patients is thus scant. Anti-TNFα antibody has recently demonstrated strong effects against recurrent uveitis in BD, but the efficacy and safety of anti-TNFα therapy in elderly patients remain unclear. We report herein the case of an elderly patient with long-standing uveitis due to BD who was successfully treated with two types of anti-TNF therapy...
2016: International Medical Case Reports Journal
Kristen Bova Campbell, Teresa A Cicci, Alyssa K Vora, Lindsey D Burgess
Colchicine is one of the oldest medications still in use today and is commonly used for the treatment of gout and familial Mediterranean fever. Its anti-inflammatory properties have raised the question of its utility in managing several cardiovascular diseases, including postoperative atrial fibrillation and pericarditis. This article will review the evidence for colchicine in these conditions and provide recommendations for use.
November 2015: Hospital Pharmacy
Anna Ulyanova, Xuan Vinh To, A B M A Asad, Weiping Han, Kai-Hsiang Chuang
Hypothalamus plays the central role in regulating energy homeostasis. To understand the hypothalamic neurocircuit in responding to leptin, Manganese-Enhanced MRI (MEMRI) was applied. Highly elevated signal could be mapped in major nuclei of the leptin signaling pathway, including the arcuate nucleus (ARC), paraventricular nucleus (PVN), ventromedial hypothalamus (VMH) and dorsomedial hypothalamus (DMH) in fasted mice and the enhancement was reduced by leptin administration. However, whether changes in MEMRI signal reflect Ca(2+) channel activity, neuronal activation or connectivity in the leptin signaling pathway are not clear...
October 8, 2016: NeuroImage
Emine Polat, Nilden Tuygun, Halise Akca, Can Demir Karacan
BACKGROUND: Colchicine poisoning is an uncommon but serious form of drug intoxication. It may produce life-threatening systemic effects. In toxic doses it produces nausea and vomiting and bone marrow suppression, often leading to sepsis, hypocalcemia, adult respiratory distress syndrome, and direct cardiotoxic effects. OBJECTIVE: The aim of this study was to describe demographic features and the outcome of patients poisoned with colchicine. METHODS: A retrospective study of the pediatric intensive care unit database was performed for patients ≤18 years of age who had colchicine poisoning between July 2008 and July 2013...
October 7, 2016: Journal of Emergency Medicine
Shin-Ichi Nureki, Koji Ishii, Hideaki Fujisaki, Masataka Torigoe, Keisuke Maeshima, Hirotaka Shibata, Eishi Miyazaki, Jun-Ichi Kadota
A 42-year-old woman presented with an intermittent fever and chest and back pain, and an abnormal chest shadow was detected. She was diagnosed with paragonimiasis caused by Paragonimus westermani. Praziquantel therapy improved the abnormal chest shadow, but did not relieve her symptoms. She was also diagnosed with familial Mediterranean fever (FMF), and colchicine therapy resolved her symptoms. She subsequently developed arthralgia and morning stiffness in her hands. We also diagnosed the patient with rheumatoid arthritis (RA), and corticosteroid and salazosulfapyridine therapy improved her symptoms...
2016: Internal Medicine
Salwa Elmeligie, Nadia Abdalla Khalil, Eman Mohamed Ahmed, Soha Hussein Emam, Sawsan Abo-Bakr Zaitone
A series of pyrazoline derivatives 2a-e, 3a-e and 4a-e structurally related to combretastatin A4 (CA-4) were synthesized and characterized by spectroscopic means and elemental analyses. In these compounds, the cis double bond of CA-4 was replaced with the pyrazoline ring aiming to enhance the cytotoxic effects displayed by CA-4 and to prevent the cis/trans isomerization that is associated with inactivation of CA-4. The cytotoxic activity of all new compounds was investigated in vitro against MCF-7 and HCT-116 cell lines...
2016: Biological & Pharmaceutical Bulletin
Massimo Imazio, Elena Gribaudo, Fiorenzo Gaita
Recurrent pericarditis is the most common and troublesome complication of pericarditis affecting 20 to 50% of patients. Its pathogenesis is often presumed to be immune-mediated, but additional investigations are needed to clarify the pathogenesis in order to develop etiology-oriented therapies. Imaging with Computed Tomography and especially Cardiac Magnetic Resonance holds promise to help in the identification of more difficult cases and improve their management. Refractory recurrent pericarditis with corticosteroid dependence and colchicine resistance remain still an unsolved issue in search of new therapies, although old drugs such as azathioprine, intravenous immunoglobulins, and biological agents seem promising, but new randomized clinical trials are needed to confirm their role...
October 7, 2016: Progress in Cardiovascular Diseases
Mehmet Akif Öztürk, Rıdvan Mercan, Kevser Gök, Ahmet Mesut Onat, Bünyamin Kısacık, Gezmiş Kimyon, Ayşe Balkarlı, Arif Kaya, Veli Çobankara, Mehmet Ali Balcı, ÖmerNuri Pamuk, Gözde Yıldırım Çetin, Mehmet Sayarlıoğlu, Soner Şenel, Mehmet Engin Tezcan, Adem Küçük, Kemal Üreten, Şafak Şahin, Abdurrahman Tufan
Although gout is potentially curable, the management of this disease is often suboptimal. In this study, we investigated the treatment of gout in Turkey and also compared the management approaches to gout in different clinical specialties. Three hundred and nineteen consecutive patients (mean age 58.60 ± 12.8 years; 44 females, 275 males) were included in this multicenter study. A standardized form was generated to collect data about the patient's first admission to health care, the specialty of the doctor first diagnosed the gout, the treatment options for gout including attack management, patient referral, chronic treatment including medical treatment, and life style modifications...
October 8, 2016: Clinical Rheumatology
Panhu Zhu, Wenfeng Ye, Jiaming Li, Yanchun Zhang, Weijun Huang, Mohan Cheng, Yujun Wang, Yang Zhang, Huicai Liu, Jian Zuo
A novel class of tetrahydroisoquinoline derivatives were designed and synthesized as antitumor agents and evaluated for their in vitro and in vivo biological activities. The antiproliferative activities of all the target compounds on HUVEC, MCF-7 and HT-29 were evaluated. Compared with Colchicine (1.04×10(-2) μM), 17d and 17e exhibited outstanding activity on MCF-7 with IC50 values 0.26×10(-2) μM and 0.89×10(-3) μΜ in cell cytotoxicity assay. The tubulin polymerization assay demonstrated that 17d and 17e exhibited better inhibition rate...
September 26, 2016: Chemical Biology & Drug Design
Junyu Wu, Zhimin He, Da-Liang Wang, Fang-Lin Sun
Microtubules play essential roles in mitosis, cell migration, and intracellular trafficking. Drugs that target microtubules have demonstrated great clinical success in cancer treatment due to their capacity to impair microtubule dynamics in both mitotic and interphase stages. In a previous report, we demonstrated that JMJD5 associated with mitotic spindle and was required for proper mitosis. However, it remains elusive whether JMJD5 could regulate the stability of cytoskeletal microtubules and whether it affects the efficacy of microtubule-targeting agents...
October 7, 2016: Cell Cycle
Jana Van Wabeke, Eric Dhondt, Isabelle Peene, Yves Piette
Gout is a common cause of inflammatory arthritis. The classical treatment options in an acute gout attack are non-steroidal anti-inflammatory drugs, colchicine, and corticosteroids. Interleukin-1 inhibition has been shown to be an effective alternative when non-biologic therapies are ineffective or contraindicated. Herein, we report the case of a 69-year-old female who presented with polyarticular tophaceous gout treated successfully with anakinra.
October 7, 2016: Acta Clinica Belgica
Kyoko Nakagawa-Goto, Yukako Taniguchi, Yurie Watanabe, Akifumi Oda, Emika Ohkoshi, Ernest Hamel, Kuo-Hsiung Lee, Masuo Goto
Previously synthesized 2-(benzo[b]thiophene-3'-yl)-6,8,8-triethyldesmosdumotin B (1, TEDB-TB) and 2-(naphth-1'-yl)-6,8,8-triethyldesmosdumotin B (2) showed potent activity against multiple human tumor cell lines, including a multidrug-resistant (MDR) subline, by targeting spindle formation and/or the microtubule network. Consequently, ester analogues of hydroxylated naphthyl substituted TEBDs (3-5) were prepared and evaluated for their effects on tumor cell proliferation and on tubulin assembly. Among all new compounds, compound 6, a 4'-acetoxynaphthalen-1'-yl derivative, displayed the most potent antiproliferative activity (IC50 0...
September 25, 2016: Bioorganic & Medicinal Chemistry
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