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niclosamide

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https://www.readbyqxmd.com/read/29113805/octenylsuccinate-hydroxypropyl-phytoglycogen-enhances-the-solubility-and-in-vitro-antitumor-efficacy-of-niclosamide
#1
Ying Xie, Yuan Yao
Niclosamide is a promising antitumor agent, but its low aqueous solubility places limit on its antitumor efficacy. The aim of this study was to improve the solubility and dissolution of niclosamide through using octenylsuccinate hydroxypropyl phytoglycogen (OHPP), an amphiphilic dendrimer-like biopolymer. The niclosamide-OHPP solid dispersion (niclo-OHPP SD) was prepared and characterized in terms of crystallinity, molecular interactions, solubility and dissolution profile, in-vitro antitumor efficacy, and in-vitro transdermal amount...
November 4, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29113501/fabrication-of-niclosamide-loaded-solid-lipid-nanoparticles-in-vitro-characterization-and-comparative-in-vivo-evaluation
#2
Maqsood Ur Rehman, Mir Azam Khan, Waheed S Khan, Muhammad Shafique, Munasib Khan
Niclosamide (NCS) is an oral anthelminthic drug having low solubility and hence low bioavailability. Current investigation shows an approach to fabricate solid lipid nanoparticles (SLNs) of NCS and evaluated for pharmaceutical, in vitro and in vivo characterization. NFM-3 showed particle size 204.2 ± 2.2 nm, polydispersity index 0.328 ± 0.02 and zeta potential -33.16 ± 2 mV. Entrapment efficiency and drug loading capacity were 84.4 ± 0.02% and 5.27 ± 0.03%, respectively. Scanning electron microscopy image indicated that particles were nanoranged...
November 7, 2017: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/29046937/field-evaluation-of-a-novel-molluscicide-niclosamidate-against-oncomelania-hupensis-intermediate-host-of-schistosoma-japonicum
#3
Weisi Wang, Xia Zhang, Huaming Zhang, Hehua Hu, Shizhu Li, Xiong Liu, Liping Duan
The molluscicidal activity of a novel molluscicide (niclosamidate) was evaluated in field trials against Oncomelania hupensis, the intermediate host of Schistosoma japonicum. The environmental safety of niclosamidate for local fishes was also studied under field conditions. The results showed that, at the dosages of 8.0 g/m(2) and 4.0 g/m(3), niclosamidate exhibits highly potent molluscicidal activity in the spraying and immersion trials, resulting in mortality rates of up to 81.8 and 72.7%, respectively...
October 18, 2017: Parasitology Research
https://www.readbyqxmd.com/read/29031202/targeting-of-cell-cycle-and-let-7a-stat3-pathway-by-niclosamide-inhibits-proliferation-migration-and-invasion-in-oral-squamous-cell-carcinoma-cells
#4
Xiaoxu Li, Ruiyu Ding, Zewen Han, Zeyun Ma, Yixiang Wang
The low median survival rate of oral squamous cell carcinoma (OSCC) is associated with chemotherapeutic resistance. Niclosamide is an oral anti-helminthic drug, its anti-cancer effect has been reported in recent years. However, the effect of niclosamide on OSCC remains largely unknown. In this study, we, for the first time, investigated the underlying mechanisms from cell cycle arrest and let-7a/STAT3 axis through CCK-8, cell cycle, apoptosis, wound healing, Transwell invasion, generation of stable cell line, real-time PCR, and western blot assays using two OSCC cell lines WSU-HN6 and Tca83...
October 11, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28978032/vitamin-c-and-doxycycline-a-synthetic-lethal-combination-therapy-targeting-metabolic-flexibility-in-cancer-stem-cells-cscs
#5
Ernestina Marianna De Francesco, Gloria Bonuccelli, Marcello Maggiolini, Federica Sotgia, Michael P Lisanti
Here, we developed a new synthetic lethal strategy for further optimizing the eradication of cancer stem cells (CSCs). Briefly, we show that chronic treatment with the FDA-approved antibiotic Doxycycline effectively reduces cellular respiration, by targeting mitochondrial protein translation. The expression of four mitochondrial DNA encoded proteins (MT-ND3, MT-CO2, MT-ATP6 and MT-ATP8) is suppressed, by up to 35-fold. This high selection pressure metabolically synchronizes the surviving cancer cell sub-population towards a predominantly glycolytic phenotype, resulting in metabolic inflexibility...
September 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28969776/the-efficacy-of-the-supramolecular-complexes-of-niclosamide-obtained-by-mechanochemical-technology-and-targeted-delivery-against-cestode-infection-of-animals
#6
Ivan A Arkhipov, Konstantin M Sadov, Yulia V Limova, Alexandra K Sadova, Anastasiya I Varlamova, Salavat S Khalikov, Alexandr V Dushkin, Yulia S Chistyachenko
Niclosamide is an anthelmintic that is widely used to treat cestode infection of animals. The efficacy of the supramolecular complexes of niclosamide obtained by mechanochemical technology and targeted delivery was studied in hymenolepiosis of mice and monieziosis of sheep. The efficacy of new substances of niclosamide with polyvinylpyrrolidone polymer in different ratios (1:10; 1:5; 1:2) was determined by the results of helminthological necropsy of the small intestine of sheep and mice. Pre-treatment eggs per gram (EPG) were not significantly different (P>0...
November 15, 2017: Veterinary Parasitology
https://www.readbyqxmd.com/read/28903339/ing5-knockdown-enhances-migration-and-invasion-of-lung-cancer-cells-by-inducing-emt-via-egfr-pi3k-akt-and-il-6-stat3-signaling-pathways
#7
Xin-Li Liu, Xu-Tao Zhang, Jin Meng, Hong-Fei Zhang, Yong Zhao, Chen Li, Yang Sun, Qi-Bing Mei, Feng Zhang, Tao Zhang
ING5 belongs to the Inhibitor of Growth (ING) candidate tumor suppressor family, whose functions have been involved in the regulation of chromatin remodeling, cell cycle progression, proliferation and apoptosis. Our previous study has shown that ING5 overexpression inhibits lung cancer aggressiveness via suppressing epithelial to mesenchymal transition (EMT). However, the mechanisms remain largely unknown. In the current study, by Phospho-Kinase array and western blot, we have defined significantly upregulated EGFR/PI3K/Akt and IL-6/STAT3 oncogenic signaling pathways in ING5 knockdown A549 cells, which could be downregulated by ING5 overexpression...
August 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28877265/niclosamide-induces-protein-ubiquitination-and-inhibits-multiple-pro-survival-signaling-pathways-in-the-human-glioblastoma-u-87-mg-cell-line
#8
Benxu Cheng, Liza Doreen Morales, Yonghong Zhang, Shizue Mito, Andrew Tsin
Glioblastoma is the most common and lethal malignant primary brain tumor for which the development of efficacious chemotherapeutic agents remains an urgent need. The anti-helminthic drug niclosamide, which has long been in use to treat tapeworm infections, has recently attracted renewed interest due to its apparent anticancer effects in a variety of in vitro and in vivo cancer models. However, the mechanism(s) of action remains to be elucidated. In the present study, we found that niclosamide induced cell toxicity in human glioblastoma cells corresponding with increased protein ubiquitination, ER stress and autophagy...
2017: PloS One
https://www.readbyqxmd.com/read/28861168/inhibition-of-wnt-%C3%AE-catenin-by-anthelmintic-drug-niclosamide-effectively-targets-growth-survival-and-angiogenesis-of-retinoblastoma
#9
Zhi Li, Qin Li, Genguo Wang, Yi Huang, Xiaochun Mao, Yanfang Zhang, Xueyan Wang
Retinoblastoma is an angiogenesis-dependent ocular tumor, the clinical management of which remains a challenge. Agents that can target tumor cells and angiogenesis, as well as augment current chemotherapy efficacy, present a promising therapeutic strategy for retinoblastoma. We demonstrated that niclosamide, an FDA-approved anthelmintic drug, is effective against multiple aspects of retinoblastoma. Niclosamide inhibited proliferation via causing cell cycle arrest at the G2/M phase and induced caspase-dependent apoptosis in a panel of retinoblastoma cell lines, including Y79, RB116, and WERI-Rb-1...
2017: American Journal of Translational Research
https://www.readbyqxmd.com/read/28828438/niclosamide-conjugated-polypeptide-nanoparticles-inhibit-wnt-signaling-and-colon-cancer-growth
#10
Jayanta Bhattacharyya, Xiu-Rong Ren, Robert A Mook, Jiangbo Wang, Ivan Spasojevic, Richard T Premont, Xinghai Li, Ashutosh Chilkoti, Wei Chen
Abnormal Wnt activity is a major mechanism responsible for many diseases, including cancer. Previously, we reported that the anthelmintic drug Niclosamide (NIC) inhibits Wnt/β-catenin signaling and suppresses colon cancer cell growth. Although the pharmacokinetic properties of NIC are appropriate for use as an anthelmintic agent, its low solubility, low bioavailability and low systemic exposure limit its usefulness in treating systemic diseases. To overcome these limitations, we conjugated NIC to recombinant chimeric polypeptides (CPs), and the CP-NIC conjugate spontaneously self-assembled into sub-100 nm near-monodisperse nanoparticles...
August 31, 2017: Nanoscale
https://www.readbyqxmd.com/read/28813646/antihelminthic-drug-niclosamide-inhibits-cip2a-and-reactivates-tumor-suppressor-protein-phosphatase-2a-in-non-small-cell-lung-cancer-cells
#11
Myeong-Ok Kim, Min Ho Choe, Yi Na Yoon, Jiyeon Ahn, Minjin Yoo, Kwan-Young Jung, Sungkwan An, Sang-Gu Hwang, Jeong Su Oh, Jae-Sung Kim
Protein phosphatase 2A (PP2A) is a critical tumor suppressor complex responsible for the inactivation of various oncogenes. Recently, PP2A reactivation has emerged asan anticancer strategy. Cancerous inhibitor of protein phosphatase 2A (CIP2A), an endogenous inhibitor of PP2A, is upregulated in many cancer cells, including non-small cell lung cancer (NSCLC) cells. We demonstrated that the antihelminthic drug niclosamide inhibited the expression of CIP2A and reactivated the tumor suppressor PP2A in NSCLC cells...
November 15, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28793917/molluscicidal-activity-and-mechanism-of-toxicity-of-a-novel-salicylanilide-ester-derivative-against-biomphalaria-species
#12
Ping He, Weisi Wang, Benjamin Sanogo, Xin Zeng, Xi Sun, Zhiyue Lv, Dongjuan Yuan, Liping Duan, Zhongdao Wu
BACKGROUND: Schistosomiasis mansoni is one of the most important, but often neglected, tropical diseases transmitted by snails of the genus Biomphalaria. Control of the intermediate host snail plays a crucial role in preventing the spread of schistosomiasis. However, there is only one molluscicide, niclosamide, recommended by the World Health Organization. Niclosamide has been used for several decades but is toxic to non-target organisms. Therefore, it is necessary to optimize the scaffold of niclosamide and develop novel molluscicides with enhanced potency and decreased toxicity to non-target organisms...
August 10, 2017: Parasites & Vectors
https://www.readbyqxmd.com/read/28780747/niclosamide-piperazine-prevents-high-fat-diet-induced-obesity-and-diabetic-symptoms-in-mice
#13
Jingjing Guo, Hanlin Tao, Amer Alasadi, Qingrong Huang, Shengkan Jin
PURPOSE: Obesity and type 2 diabetes (T2D) have become the major public health challenges globally. Mitochondrial uncoupling, which reduces intracellular lipid loads and corrects the underlying cause of insulin resistance, has emerged as a promising anti-obese and anti-diabetic intervention. Niclosamide is an anthelmintic drug approved by the US FDA with the mechanism of action that uncouples mitochondria of parasitic worms. Recently, niclosamide ethanolamine salt (NEN) was found to be a safe and effective hepatic mitochondrial uncoupler for the prevention and treatment of obesity and T2D in mouse models...
August 5, 2017: Eating and Weight Disorders: EWD
https://www.readbyqxmd.com/read/28685770/existing-drugs-as-broad-spectrum-and-potent-inhibitors-for-zika-virus-by-targeting-ns2b-ns3-interaction
#14
Zhong Li, Matthew Brecher, Yong-Qiang Deng, Jing Zhang, Srilatha Sakamuru, Binbin Liu, Ruili Huang, Cheri A Koetzner, Christina A Allen, Susan A Jones, Haiying Chen, Na-Na Zhang, Min Tian, Fengshan Gao, Qishan Lin, Nilesh Banavali, Jia Zhou, Nathan Boles, Menghang Xia, Laura D Kramer, Cheng-Feng Qin, Hongmin Li
Recent outbreaks of Zika virus (ZIKV) highlight an urgent need for therapeutics. The protease complex NS2B-NS3 plays essential roles during flaviviral polyprotein processing, and thus represents an attractive drug target. Here, we developed a split luciferase complementation-based high-throughput screening assay to identify orthosteric inhibitors that directly target flavivirus NS2B-NS3 interactions. By screening a total of 2 816 approved and investigational drugs, we identified three potent candidates, temoporfin, niclosamide, and nitazoxanide, as flavivirus NS2B-NS3 interaction inhibitors with nanomolar potencies...
August 2017: Cell Research
https://www.readbyqxmd.com/read/28675238/indirect-photodegradation-of-the-lampricides-tfm-and-niclosamide
#15
Megan B McConville, Stephen P Mezyk, Christina K Remucal
3-Trifluromethyl-4-nitrophenol (TFM) and 2',5-dichloro-4'-nitrosalicylanilide (niclosamide) are lampricides used in tributaries of the Great Lakes to kill the invasive parasitic sea lamprey (Petromyzon marinus). Although the lampricides have been applied since the late 1950s, their photochemical behavior in natural environments is still not well understood. This study examines the indirect photodegradation of these two compounds and the resulting yields of organic and inorganic photoproducts in water samples collected from five tributaries of Lake Michigan...
August 16, 2017: Environmental Science. Processes & Impacts
https://www.readbyqxmd.com/read/28642838/adaptive-pathways-and-emerging-strategies-overcoming-treatment-resistance-in-castration-resistant-prostate-cancer
#16
Cameron M Armstrong, Allen C Gao
The therapies available for prostate cancer patients whom progress from hormone-sensitive to castration resistant prostate cancer include both systemic drugs, including docetaxel and cabazitaxel, and drugs that inhibit androgen signaling such as enzalutamide and abiraterone. Unfortunately, it is estimated that up to 30% of patients have primary resistance to these treatments and over time even those who initially respond to therapy will eventually develop resistance and their disease will continue to progress regardless of the presence of the drug...
October 2016: Asian Journal of Urology
https://www.readbyqxmd.com/read/28634145/taeniasis-caused-by-taenia-saginata-in-gianyar-town-and-taenia-solium-in-karangasem-villages-of-bali-indonesia-2011-2016-how-to-detect-tapeworm-carriers-anamnesis-or-microscopy
#17
Kadek Swastika, Toni Wandra, Nyoman Sadra Dharmawan, I Made Sudarmaja, John Master Saragih, Luh Putu Eka Diarthini, Luh Ariwati, Putu Ayu Asri Damayanti, Dewa Ayu Agus Sri Laksemi, Nengah Kapti, Putu Sutisna, Tetsuya Yanagida, Akira Ito
From January 2011 until September 2016, screening of taeniasis carriers was carried out in a town in Gianyar District (Taenia saginata) and in villages which consisted of several Banjars (the smallest community units) on the eastern slope of Mt. Agung, Karangasem District (Taenia solium) in Bali, Indonesia. Fecal samples from all community members who chose to participate were examined microscopically for detection of taeniid eggs each person completedwith a questionnaire to determine if they had seen whitish, noodle-like proglottids (anamnesis) in their feces...
June 17, 2017: Acta Tropica
https://www.readbyqxmd.com/read/28632878/identification-of-novel-g-protein-coupled-receptor-143-ligands-as-pharmacologic-tools-for-investigating-x-linked-ocular-albinism
#18
Elisabetta De Filippo, Prashiela Manga, Anke C Schiedel
Purpose: GPR143 regulates melanosome biogenesis and organelle size in pigment cells. The mechanisms underlying receptor function remain unclear. G protein-coupled receptors (GPCRs) are excellent pharmacologic targets; thus, we developed and applied a screening approach to identify potential GPR143 ligands and chemical modulators. Methods: GPR143 interacts with β-arrestin; we therefore established a β-arrestin recruitment assay to screen for compounds that modulate activity...
June 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/28627643/niclosamide-attenuates-inflammatory-cytokines-via-the-autophagy-pathway-leading-to-improved-outcomes-in-renal-ischemia-reperfusion-injury
#19
Lin-Xia Zhang, Hui-Juan Zhao, Dong-Li Sun, Shan-Lin Gao, Hong-Mei Zhang, Xin-Guo Ding
Renal ischemia/reperfusion (I/R) injury is a debilitating condition that leads to loss renal function and damage to kidney tissue in the majority of patients with acute kidney disease. Previous studies have indicated that autophagy serves a protective function in renal I/R injury. In the present study, the effect of the anthelmintic niclosamide in the regulation of inflammatory responses in kidney I/R was investigated. A total of 40 Sprague-Dawley rats were randomly divided into the following 5 groups (n=8 in each group): Sham group; renal I/R injury; renal I/R injury plus 3‑methyladenine (3‑MA) treatment (15 mg/kg); renal I/R injury plus niclosamide (25 mg/kg); and renal I/R injury plus rapamycin (10 mg/kg)...
August 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28622697/vitamin-c-and-doxycycline-a-synthetic-lethal-combination-therapy-targeting-metabolic-flexibility-in-cancer-stem-cells-cscs
#20
Ernestina Marianna De Francesco, Gloria Bonuccelli, Marcello Maggiolini, Federica Sotgia, Michael P Lisanti
Here, we developed a new synthetic lethal strategy for further optimizing the eradication of cancer stem cells (CSCs). Briefly, we show that chronic treatment with the FDA-approved antibiotic Doxycycline effectively reduces cellular respiration, by targeting mitochondrial protein translation. The expression of four mitochondrial DNA encoded proteins (MT-ND3, MT-CO2, MT-ATP6 and MT-ATP8) is suppressed, by up to 35-fold. This high selection pressure metabolically synchronizes the surviving cancer cell sub-population towards a predominantly glycolytic phenotype, resulting in metabolic inflexibility...
June 9, 2017: Oncotarget
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