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https://www.readbyqxmd.com/read/28615941/development-and-optimization-of-an-injectable-formulation-of-copper-diethyldithiocarbamate-an-active-anticancer-agent
#1
Mohamed Wehbe, Malathi Anantha, Minghan Shi, Ada Wai-Yin Leung, Wieslawa H Dragowska, Léon Sanche, Marcel B Bally
Copper diethyldithiocarbamate (Cu(DDC)2) is the active anticancer agent generated when disulfiram (DSF) is provided in the presence of copper. To date, research directed toward repurposing DSF as an anticancer drug has focused on administration of DSF and copper in combination, efforts that have proven unsuccessful in clinical trials. This is likely due to the inability to form Cu(DDC)2 at relevant concentrations in regions of tumor growth. Little effort has been directed toward the development of Cu(DDC)2 because of the inherent aqueous insolubility of the complex...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28595020/tamoxifen-inhibits-mitochondrial-membrane-damage-caused-by-disulfiram
#2
Natalia Pavon, Mabel Buelna-Chontal, Francisco Correa, Belem Yoval-Sánchez, Javier Belmont, Luz Hernández-Esquivel, Jose S Rodríguez-Zavala, Edmundo Chavez
In this work, we studied the protective effect of tamoxifen on disulfiram-induced mitochondrial membrane insult. The results indicate that tamoxifen circumvents inner membrane leakiness manifested by Ca2+ release, mitochondrial swelling, and collapse of the transmembrane electric gradient. Furthermore, it was found that tamoxifen prevents the inactivation of the mitochondrial enzyme aconitase and detachment of cytochrome c from the inner membrane. Interestingly, tamoxifen also inhibited disulfiram-promoted generation of hydrogen peroxide...
June 8, 2017: Biochemistry and Cell Biology, Biochimie et Biologie Cellulaire
https://www.readbyqxmd.com/read/28528648/copper-and-antibiotics-discovery-modes-of-action-and-opportunities-for-medicinal-applications
#3
Alex G Dalecki, Cameron L Crawford, Frank Wolschendorf
Copper is a ubiquitous element in the environment as well as living organisms, with its redox capabilities and complexation potential making it indispensable for many cellular functions. However, these same properties can be highly detrimental to prokaryotes and eukaryotes when not properly controlled, damaging many biomolecules including DNA, lipids, and proteins. To restrict free copper concentrations, all bacteria have developed mechanisms of resistance, sequestering and effluxing labile copper to minimize its deleterious effects...
2017: Advances in Microbial Physiology
https://www.readbyqxmd.com/read/28527633/anthelmintic-activity-of-cytochrome-p450-inhibitors-miconazole-and-clotrimazole-in-vitro-effect-on-the-liver-fluke-opisthorchis-felineus
#4
Viatcheslav A Mordvinov, Alexander G Shilov, Maria Y Pakharukova
Discovery of drugs for the treatment of opisthorchiasis and schistosomiasis is a high priority. The basic metabolic cytochrome P450 (CYP) system in parasitic flatworms contains a single gene. CYP of the liver fluke Opisthorchis felineus, the causative agent of opisthorchiasis, is important for survival of the worm, so it may be a promising target for therapeutics against liver fluke infection. The aims of this study were: (i) to analyse in-vitro anthelmintic activity of various CYP inhibitors using standard motility and mortality assays against juvenile and adult O...
May 17, 2017: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28518151/disulfiram-copper-selectively-eradicates-aml-leukemia-stem-cells-in-vitro-and-in-vivo-by-simultaneous-induction-of-ros-jnk-and-inhibition-of-nf-%C3%AE%C2%BAb-and-nrf2
#5
Bing Xu, Shiyun Wang, Rongwei Li, Kai Chen, Lingli He, Manman Deng, Vinodh Kannappan, Jie Zha, Huijuan Dong, Weiguang Wang
Acute myeloid leukemia (AML) is a heterogeneous malignancy. Despite the advances in past decades, the clinical outcomes of AML patients remain poor. Leukemia stem cells (LSCs) is the major cause of the recurrence of AML even after aggressive treatment making, promoting development of LSC-targeted agents is an urgent clinical need. Although the antitumor activity of disulfiram (DS), an approved anti-alcoholism drug, has been demonstrated in multiple types of tumors including hematological malignancies such as AML, it remains unknown whether this agent would also be able to target cancer stem cells like LSCs...
May 18, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28490767/biliverdin-reductase-inhibitors-did-not-improve-severe-unconjugated-hyperbilirubinemia-in-vivo
#6
Remco van Dijk, Sem J Aronson, Dirk R de Waart, Stan F van de Graaf, Suzanne Duijst, Jurgen Seppen, Ronald Oude Elferink, Ulrich Beuers, Piter J Bosma
We aimed to identify potent biliverdin reductase (BVRA) inhibitors as a novel concept for the treatment of severe unconjugated hyperbilirubinemia. 1280 FDA-approved compounds were screened in vitro for their ability to inhibit human and rat BVRA activity and 26 compounds were identified as BVRA inhibitors. Montelukast and Disulfiram were selected as potentially clinically applicable drugs and tested to reduce serum unconjugated bilirubin (UCB) levels in the Ugt1a1-deficient rat, a model for chronic unconjugated hyperbilirubinemia...
May 10, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28465838/a-critical-review-of-the-evidence-concerning-the-hiv-latency-reversing-effect-of-disulfiram-the-possible-explanations-for-its-inability-to-reduce-the-size-of-the-latent-reservoir-in-vivo-and-the-caveats-associated-with-its-use-in-practice
#7
REVIEW
Harry D J Knights
Combination antiretroviral therapy (cART) effectively suppresses the replication of human immunodeficiency virus type 1 (HIV-1), improves immune function, and decreases the morbidity of acquired immune deficiency syndrome (AIDS). However, it is unable to eradicate the virus because it does not eliminate latently infected cells. The latent reservoir poses the major barrier to an HIV-1 cure. The "shock and kill" strategy aims to reactivate the virus and destroy latently infected cells. Many latency reversing agents (LRAs) reactivate HIV in vitro, but the absence of damaging side-effects and efficacy in vivo make disulfiram particularly promising...
2017: AIDS Research and Treatment
https://www.readbyqxmd.com/read/28460441/inflammatory-breast-cancer-tumor-emboli-express-high-levels-of-anti-apoptotic-proteins-use-of-a-quantitative-high-content-and-high-throughput-3d-ibc-spheroid-assay-to-identify-targeting-strategies
#8
Jay Arora, Scott J Sauer, Michael Tarpley, Peter Vermeulen, Charlotte Rypens, Steven Van Laere, Kevin P Williams, Gayathri R Devi, Mark W Dewhirst
Inflammatory breast cancer (IBC) is one of the most lethal breast cancer variants; with existing therapy, 5-yr survival rate is only 35%. Current barriers to successful treatment of IBC include frequent infiltration and the presence of tumor cell clusters, termed tumor emboli, within the breast parenchyma and lymphatics. Prior studies have identified the role of anti-apoptotic signaling, in particular hyperactivation of NFκB and its target genes, in IBC pathobiology and therapeutic resistance. The objectives of this study were to: (1) determine if IBC tumor emboli express anti-apoptotic proteins and (2) develop a high content, multiparametric assay to assess the morphology of the IBC 3D spheroids and to optimize a high throughput format to screen for compounds that can inhibit the formation of the IBC tumor clusters/embolic structures...
April 18, 2017: Oncotarget
https://www.readbyqxmd.com/read/28440205/in-vitro-collapsing-colon-cancer-cells-by-selectivity-of-disulfiram-loaded-charge-switchable-nanoparticles-against-cancer-stem-cells
#9
Marwa Muhammad Abu-Serie, Fatma Hassan El-Rashidy
BACKGROUND: Different strategies against colon cancer are accompanied by treatment failure, because of drug toxicity toward normal cells and cancer stem cells (CSCs) resistance. However, previous patent evaluated liposome that encapsulated inhibitor of CSCs' aldehyde dehydrogenase (ALDH)1; disulfiram, for targeting breast CSCs. Liposome has disadvantages due to its hydrophobicity. OBJECTIVES: Designing hydrophilic nanoparticles have selectivity to release disulfiram in CC cells rather than in normal colonocytes based on variation in microenvironment between normal and cancer cells...
April 24, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/28406579/disparities-in-pharmacotherapy-for-alcohol-use-disorder-in-the-context-of-universal-health-care-a-swedish-register-study
#10
Katherine J Karriker-Jaffe, Jianguang Ji, Jan Sundquist, Kenneth S Kendler, Kristina Sundquist
BACKGROUND AND AIMS: Pharmacotherapy can be an important part of the continuum of care for alcohol use disorder (AUD). The Swedish universal health-care system emphasizes provision of care to marginalized groups. The primary aim was to test associations of neighborhood deprivation and disadvantaged social status with receipt of AUD pharmacotherapy in this context. DESIGN: Data from linked population registers were used to follow an open cohort over 7 years. SETTING: Sweden...
April 12, 2017: Addiction
https://www.readbyqxmd.com/read/28373070/disulfiram-suppresses-cancer-stem-like-properties-and-stat3-signaling-in-triple-negative-breast-cancer-cells
#11
Yoon-Jae Kim, Ji Young Kim, Nahyun Lee, Eunhye Oh, Daeil Sung, Tae-Min Cho, Jae Hong Seo
In the presence of copper (Cu), disulfiram (DSF) suppresses properties associated with cancer stem cells (CSCs) in breast cancer, but the mechanism of action is poorly understood. In the present study, we observed that DSF/Cu treatment induced apoptosis, mediated by caspase-3 activation in triple-negative breast cancer (TNBC) cells. DSF/Cu treatment also specifically targeted CSC-like cell populations, marked by the inhibition of ALDH1 activity, the suppression of CD44+/CD24-and CD49f+/CD24 + subpopulations, and the subsequent impairment of mammosphere formation...
May 13, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28344087/subacute-alcohol-and-or-disulfiram-intake-affects-bioelements-and-redox-status-in-rat-testes
#12
Ana Djuric, Aida Begic, Borko Gobeljic, Ana Pantelic, Goran Zebic, Ivana Stevanovic, Dragan Djurdjevic, Milica Ninkovic, Vera Prokic, Ivan Stanojevic, Danilo Vojvodic, Mirjana Djukic
The aim of the study was to investigate if alcohol and disulfiram (DSF) individually and in combination affect bioelements' and red-ox homeostasis in testes of the exposed rats. The animals were divided into groups according to the duration of treatments (21 and/or 42 days): C21/C42 groups (controls); OL21 and OL22-42 groups (0.5 mL olive oil intake); A1-21 groups (3 mL 20% ethanol intake); DSF1-21 groups (178.5 mg DSF/kg/day intake); and A21+DSF22-42 groups (the DSF ingestion followed previous 21 days' treatment with alcohol)...
March 24, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28340172/repositioning-disulfiram-as-a-radiosensitizer-against-atypical-teratoid-rhabdoid-tumor
#13
Young Eun Lee, Seung Ah Choi, Pil Ae Kwack, Hak Jae Kim, Il Han Kim, Kyu-Chang Wang, Ji Hoon Phi, Ji Yeoun Lee, Sangjoon Chong, Sung-Hye Park, Kyung Duk Park, Do Won Hwang, Kyeung Min Joo, Seung-Ki Kim
Background.: Atypical teratoid/rhabdoid tumor (AT/RT) is one of the most common malignant brain tumors in infants. Although cancer stem cells of AT/RT express aldehyde dehydrogenase (ALDH), effective chemotherapies against AT/RT have not been established. Here, we examined radiosensitizing effects of disulfiram (DSF), an irreversible inhibitor of ALDH against AT/RT for a novel therapeutic method. Methods.: Patient-derived primary cultured AT/RT cells (SNU.AT/RT-5 and SNU...
March 17, 2017: Neuro-oncology
https://www.readbyqxmd.com/read/28319159/drug-therapy-for-alcohol-dependence-in-primary-care-in-the-uk-a-clinical-practice-research-datalink-study
#14
Andrew Thompson, Darren M Ashcroft, Lynn Owens, Tjeerd P van Staa, Munir Pirmohamed
AIM: To evaluate drug therapy for alcohol dependence in the 12 months after first diagnosis in UK primary care. DESIGN: Open cohort study. SETTING: General practices contributing data to the UK Clinical Practice Research Database. PARTICIPANTS: 39,980 people with an incident diagnosis of alcohol dependence aged 16 years or older between 1 January 1990 and 31 December 2013. MAIN OUTCOME MEASURE: Use of pharmacotherapy (acamprosate, disulfiram, naltrexone, baclofen and topiramate) to promote abstinence from alcohol or reduce drinking to safe levels in the first 12 months after a recorded diagnosis of alcohol dependence...
2017: PloS One
https://www.readbyqxmd.com/read/28301219/management-of-comorbid-bipolar-disorder-and-substance-use-disorders
#15
Ihsan M Salloum, Edson Sherwood Brown
BACKGROUND: The comorbidity of substance use disorders (SUDs) in bipolar disorder is among the highest in psychiatric disorders. Evidence-based controlled psychosocial or pharmacological interventions trials, which may guide treatment decisions, have not been systematically reviewed. OBJECTIVE: To present a narrative review of the public health and clinical significance of this condition, including diagnostic and treatment implications, and to evaluate controlled trials conducted to date...
July 2017: American Journal of Drug and Alcohol Abuse
https://www.readbyqxmd.com/read/28300663/1-2-dichloropropane-generates-phosphorylated-histone-h2ax-via-cytochrome-p450-2e1-mediated-metabolism
#16
Tatsushi Toyooka, Yukie Yanagiba, Megumi Suda, Yuko Ibuki, Rui-Sheng Wang
1,2-Dichloropropane (1,2-DCP), a synthetic chlorinated solvent, was recently classified as carcinogenic. Genotoxic events are known as a crucial step in the initiation of cancer. However, studies on the genotoxicity of 1,2-DCP are very limited, particularly studies investigating the mechanism behind DNA damage by 1,2-DCP. In this study, we examined the genotoxicity of 1,2-DCP using phosphorylated histone H2AX (γ-H2AX), a sensitive DNA damage marker. 1,2-DCP showed dose- (1-10mM: 4h) and time-dependent (1-24h: 5mM) γ-H2AX generation in cultured human hepatocytes (WRL-68) and cholangiocytes (MMNK-1)...
March 12, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28242228/protein-s-glutathionylation-alters-superoxide-hydrogen-peroxide-emission-from-pyruvate-dehydrogenase-complex
#17
Marisa O'Brien, Julia Chalker, Liam Slade, Danielle Gardiner, Ryan J Mailloux
Pyruvate dehydrogenase (Pdh) is a vital source of reactive oxygen species (ROS) in several different tissues. Pdh has also been suggested to serve as a mitochondrial redox sensor. Here, we report that O2(•-)/ H2O2 emission from pyruvate dehydrogenase (Pdh) is altered by S-glutathionylation. Glutathione disulfide (GSSG) amplified O2(•-)/ H2O2 production by purified Pdh during reverse electron transfer (RET) from NADH. Thiol oxidoreductase glutaredoxin-2 (Grx2) reversed these effects confirming that Pdh is a target for S-glutathionylation...
February 27, 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28240173/personalized-medicine-of-alcohol-addiction-pharmacogenomics-and-beyond
#18
Vangelis George Manolopoulos, Georgia Ragia
Alcohol addiction or alcoholism is the most severe form of problem drinking. A variety of treatment methods for alcoholism are currently available that combine medications, behavioral treatment and peer support. The drugs that are currently approved by the U.S. Food and Drug Administration (FDA) for treatment of alcohol dependence are disulfiram, naltrexone and acamprosate. For many patients, however, these treatments are not effective. Evidence from a number of different studies suggests that different factors, both psychosocial and economic, as well as genetic variation, are significant contributors to interindividual variation both of clinical presentation of alcohol problems and response to a given treatment...
February 23, 2017: Current Pharmaceutical Biotechnology
https://www.readbyqxmd.com/read/28220511/review-article-pharmacotherapy-for-alcohol-dependence-the-why-the-what-and-the-wherefore
#19
REVIEW
E T Goh, M Y Morgan
BACKGROUND: The development of alcohol dependence is associated with significant morbidity and mortality. For the majority of affected people the most appropriate goal, in terms of drinking behaviour, is abstinence from alcohol. Psychosocial intervention is the mainstay of the treatment but adjuvant pharmacotherapy is also available and its use recommended. AIM: To provide an updated analysis of current and potential pharmacotherapeutic options for the management of alcohol dependence...
February 20, 2017: Alimentary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28182125/disulfiram-loaded-porous-plga-microparticle-for-inhibiting-the-proliferation-and-migration-of-non-small-cell-lung-cancer
#20
Chenhui Wang, Jiebing Yang, Haobo Han, Jiawen Chen, Yudi Wang, Quanshun Li, Yanbo Wang
In this study, poly(lactic-co-glycolic acid) (PLGA) was used as a carrier to construct disulfiram-loaded porous microparticle through the emulsion solvent evaporation method, using ammonium bicarbonate as a porogen. The microparticle possessed highly porous surface, suitable aerodynamic diameter for inhalation (8.31±1.33 µm), favorable drug loading (4.09%±0.11%), and sustained release profile. The antiproliferation effect of release supernatant was detected through 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay using non-small-cell lung cancer A549 as a model, with only 13...
2017: International Journal of Nanomedicine
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