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https://www.readbyqxmd.com/read/29289673/modeling-of-a-hybrid-langmuir-adsorption-isotherm-for-describing-interactions-between-drug-molecules-and-silica-surfaces
#1
Thomas Sandberg, Christian Weinberger, Didem Şen Karaman, Jessica M Rosenholm
The interaction between disulfiram (Antabus®) and silica was studied experimentally by adsorption from apolar solvent onto highly porous silica material (Santa Barbara Amorphous material-3, SBA-3) with large surface area. The adsorption isotherm was fitted to the Langmuir model by accounting two different affinities contributing to the overall behavior, which were attributed to two different types of silanol groups (i.e. geminal and vicinal) present on amorphous silica surfaces. This assumption was supported by theoretical calculations...
December 28, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29289665/disulfiram-can-inhibit-mers-and-sars-coronavirus-papain-like-proteases-via-different-modes
#2
Min-Han Lin, David C Moses, Chih-Hua Hsieh, Shu-Chun Cheng, Yau-Hung Chen, Chiao-Yin Sun, Chi-Yuan Chou
Severe acute respiratory syndrome coronavirus (SARS-CoV) emerged in southern China in late 2002 and caused a global outbreak with a fatality rate around 10% in 2003. Ten years later, a second highly pathogenic human CoV, MERS-CoV, emerged in the Middle East and has spread to other countries in Europe, North Africa, North America and Asia. As of November 2017, MERS-CoV had infected at least 2102 people with a fatality rate of about 35% globally, and hence there is an urgent need to identify antiviral drugs that are active against MERS-CoV...
December 28, 2017: Antiviral Research
https://www.readbyqxmd.com/read/29274360/disulfiram-with-or-without-metformin-inhibits-oesophageal-squamous-cell-carcinoma-in-vivo
#3
Rupal Jivan, Jade Peres, Leonard Howard Damelin, Reubina Wadee, Robin Bruce Veale, Sharon Prince, Demetra Mavri-Damelin
Oesophageal squamous cell carcinoma (OSCC) is highly prevalent in developing countries but there has been little recent progress into efficacious yet affordable treatment strategies. Drug repurposing is one attractive approach for cancer therapy. Disulfiram (DSF), used to treat alcoholism, inhibits cancer growth and we previously found that DSF perturbs protein degradation/turnover pathways in vitro. This was enhanced by combining DSF with the anti-diabetic drug metformin (Met). Here, we investigated DSF with/without Met, against OSCC in vivo...
December 20, 2017: Cancer Letters
https://www.readbyqxmd.com/read/29273901/systematic-review-of-combined-pharmacotherapy-for-the-treatment-of-alcohol-use-disorder-in-patients-without-comorbid-conditions
#4
REVIEW
Andrew C Naglich, Austin Lin, Sidarth Wakhlu, Bryon H Adinoff
BACKGROUND: Previous reviews have examined the use of theoretically supported combinations of drugs for the treatment of alcohol use disorder. This review seeks to examine the strengths and limitations of current clinical evidence for the use of combined pharmacological interventions intended to treat alcohol use disorder. OBJECTIVES: The objective of this review was to identify combinations of pharmacological treatments for alcohol use disorder, and assess the strength of clinical evidence for these treatments...
December 22, 2017: CNS Drugs
https://www.readbyqxmd.com/read/29260197/the-intraocular-lens-as-a-drug-delivery-device-in-vitro-screening-of-pharmacologic-substances-for-the-prophylaxis-of-posterior-capsule-opacification
#5
Christian Wertheimer, Stefan Kassumeh, Nick P Piravej, Olga Nilmayer, Christian Braun, Claudia Priglinger, Nikolaus Luft, Armin Wolf, Wolfgang J Mayer, Siegfried G Priglinger, Kirsten H Eibl-Lindner
Purpose: Numerous pharmacologic substances have been proposed for preventing posterior capsule opacification (PCO). The following trial was to compare those drugs to find more suitable options. IOL should then be modified by the pharmaceuticals as a drug-delivery device. Methods: A systematic literature search was performed to identify published substances. FHL-124 was used to determine cell proliferation and toxicity using a dye reduction test (XTT). Prescreened substances showing a reduction on cell growth without being toxic were soaked into an IOL...
December 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/29247315/development-of-a-copper-clioquinol-formulation-suitable-for-intravenous-use
#6
Moe Wehbe, Armaan K Malhotra, Malathi Anantha, Cody Lo, Wieslawa H Dragowska, Nancy Dos Santos, Marcel B Bally
Clioquinol (CQ) is an FDA-approved topical antifungal agent known to kill cancer cells. This facilitated the initiation of clinical trials in patients with refractory hematologic malignancies. These repurposing efforts were not successful; this was likely due to low intracellular levels of the drug owing to poor absorption and rapid metabolism upon oral administration. CQ forms a sparingly soluble copper complex (Cu(CQ)2) that exhibits enhanced anticancer activity in some cell lines. We have utilized a novel method to synthesize Cu(CQ)2 inside liposomes, an approach that maintains the complex suspended in solution and in a format suitable for intravenous administration...
December 16, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/29247017/the-alcohol-abuse-drug-disulfiram-targets-npl4-to-exert-antitumor-effects
#7
(no author information available yet)
Disulfiram reduced cancer mortality in patients who continued disulfiram for alcohol dependency.
December 15, 2017: Cancer Discovery
https://www.readbyqxmd.com/read/29211715/alcohol-abuse-drug-disulfiram-targets-cancer-via-p97-segregase-adaptor-npl4
#8
Zdenek Skrott, Martin Mistrik, Klaus Kaae Andersen, Søren Friis, Dusana Majera, Jan Gursky, Tomas Ozdian, Jirina Bartkova, Zsofia Turi, Pavel Moudry, Marianne Kraus, Martina Michalova, Jana Vaclavkova, Petr Dzubak, Ivo Vrobel, Pavla Pouckova, Jindrich Sedlacek, Andrea Miklovicova, Anne Kutt, Jing Li, Jana Mattova, Christoph Driessen, Q Ping Dou, Jørgen Olsen, Marian Hajduch, Boris Cvek, Raymond J Deshaies, Jiri Bartek
Cancer incidence is rising and this global challenge is further exacerbated by tumour resistance to available medicines. A promising approach to meet the need for improved cancer treatment is drug repurposing. Here we highlight the potential for repurposing disulfiram (also known by the trade name Antabuse), an old alcohol-aversion drug that has been shown to be effective against diverse cancer types in preclinical studies. Our nationwide epidemiological study reveals that patients who continuously used disulfiram have a lower risk of death from cancer compared to those who stopped using the drug at their diagnosis...
December 6, 2017: Nature
https://www.readbyqxmd.com/read/29197728/disulfiram-as-a-novel-inactivator-of-giardia-lamblia-triosephosphate-isomerase-with-antigiardial-potential
#9
Adriana Castillo-Villanueva, Yadira Rufino-González, Sara-Teresa Méndez, Angélica Torres-Arroyo, Martha Ponce-Macotela, Mario Noé Martínez-Gordillo, Horacio Reyes-Vivas, Jesús Oria-Hernández
Giardiasis, the infestation of the intestinal tract by Giardia lamblia, is one of the most prevalent parasitosis worldwide. Even though effective therapies exist for it, the problems associated with its use indicate that new therapeutic options are needed. It has been shown that disulfiram eradicates trophozoites in vitro and is effective in vivo in a murine model of giardiasis; disulfiram inactivation of carbamate kinase by chemical modification of an active site cysteine has been proposed as the drug mechanism of action...
December 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29164566/drug-related-oral-malodour-halitosis-a-literature-review
#10
M Torsten, G Gómez-Moreno, A Aguilar-Salvatierra
Dry mouth (xerostomia), is a fairly common, well-researched condition, which is an indirect cause of oral malodour. This systematic literature review looked into another cause of bad breath: adverse drug reactions in the orofacial region causing halitosis. The study focused on extraoral halitosis, and its subdivisions, particularly blood borne halitosis in which malodourous compounds in the blood stream are carried to the lungs, passively diffused across the pulmonary alveolar membrane to enter the breath. An electronic search was conducted in various databases...
November 2017: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/29155365/targeting-aldh2-with-disulfiram-copper-reverses-the-resistance-of-cancer-cells-to-microtubule-inhibitors
#11
Nan-Nan Wang, Li-Hui Wang, Yi Li, Shi-Yuan Fu, Xue Xue, Li-Na Jia, Xiang-Zhong Yuan, Ya-Ting Wang, Xing Tang, Jing-Yu Yang, Chun-Fu Wu
Disulfiram (DSF) in combination with copper (Cu) has been reported to override drug resistance in cancer cells, and DSF combined with chemotherapy based on the microtubule inhibitor vinorelbine appears to prolong survival in non-small cell lung cancer patients. Here, we investigated the mechanisms underlying these findings. DSF/Cu reversed the microtubule inhibitor resistance in A549/Taxol and KB/VCR cells in vitro, and had anti-tumor effects in A549/Taxol and KB/VCR xenograft mice. DSF/Cu and DSF reduced the cancer stem cell (CSC) characteristics of drug-resistant A549/Taxol and KB/VCR cells, including sphere formation, colony generation and migration, and DSF/Cu was more effective than DSF alone...
November 16, 2017: Experimental Cell Research
https://www.readbyqxmd.com/read/29148232/disulfiram-combined-with-copper-inhibits-metastasis-and-epithelial-mesenchymal-transition-in-hepatocellular-carcinoma-through-the-nf-%C3%AE%C2%BAb-and-tgf-%C3%AE-pathways
#12
Yi Li, Li-Hui Wang, Hao-Tian Zhang, Ya-Ting Wang, Shuai Liu, Wen-Long Zhou, Xiang-Zhong Yuan, Tian-Yang Li, Chun-Fu Wu, Jing-Yu Yang
Late-stage hepatocellular carcinoma (HCC) usually has a low survival rate because of the high risk of metastases and the lack of an effective cure. Disulfiram (DSF) has copper (Cu)-dependent anticancer properties in vitro and in vivo. The present work aims to explore the anti-metastasis effects and molecular mechanisms of DSF/Cu on HCC cells both in vitro and in vivo. The results showed that DSF inhibited the proliferation, migration and invasion of HCC cells. Cu improved the anti-metastatic activity of DSF, while Cu alone had no effect...
November 17, 2017: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/29135106/evidence-for-the-efficacy-of-disulfiram-and-copper-combination-in-glioblastoma-multiforme-a-propos-of-a-case
#13
Petros N Karamanakos, Dimitrios T Trafalis, Dionysios J Papachristou, Eleftheria S Panteli, Maria Papavasilopoulou, Andreas Karatzas, Dimitrios Kardamakis, Georgios Nasioulas, Marios Marselos
Glioblastoma multiforme (GBM) is the most common and aggressive malignancy of the central nervous system. Treatment usually involves a combination of surgical resection, chemotherapy, and radiotherapy, but ultimately this condition is incurable. Besides the dismal prognosis of GBM, financial factors have also presented challenges for advancing treatments. Taking into consideration the high cost of developing new anticancer drugs as well as the fact that GBM is a rare disease, thus further limiting financial incentive for drug development, it becomes obvious that there has been growing interest for repurposing candidates...
September 2017: Journal of B.U.ON.: Official Journal of the Balkan Union of Oncology
https://www.readbyqxmd.com/read/29128392/adrenergic-manipulation-inhibits-pavlovian-conditioned-approach-behaviors
#14
Kyle Z Pasquariello, Marina Han, Cagla Unal, Paul J Meyer
Environmental rewards and Pavlovian reward cues can acquire incentive salience, thereby eliciting incentive motivational states and instigate reward-seeking. In rats, the incentive salience of food cues can be measured during a Pavlovian conditioned approach paradigm, in which rats engage in cue-directed approach ("sign-tracking") or approach the food delivery location ("goal-tracking"). While it has been shown that dopamine signaling is necessary for sign-tracking, some studies have suggested that norepinephrine is involved in learning to sign-track as well...
November 8, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/29120249/alcohol-addiction-the-safety-of-available-approved-treatment-options
#15
Mariangela Antonelli, Anna Ferrulli, Luisa Sestito, Gabriele A Vassallo, Claudia Tarli, Carolina Mosoni, Maria M Rando, Antonio Mirijello, Antonio Gasbarrini, Giovanni Addolorato
Alcohol Use Disorders (AUD) is a leading cause of mortality and morbidity worldwide. At present disulfiram, naltrexone and acamprosate are approved for the treatment of AUD in U.S. and Europe. Nalmefene is approved in Europe and sodium oxybate is approved in Italy and Austria only. Baclofen received a 'temporary recommendation for use' in France. Areas covered: The safety of the above mentioned medications on liver, digestive system, kidney function, nervous system, pregnancy and lactation and their possible side effects are described and discussed...
November 20, 2017: Expert Opinion on Drug Safety
https://www.readbyqxmd.com/read/29069808/targeting-the-cancer-stem-cell-marker-aldehyde-dehydrogenase-1-to-circumvent-cisplatin-resistance-in-nsclc
#16
Lauren MacDonagh, Michael F Gallagher, Brendan Ffrench, Claudia Gasch, Eamon Breen, Steven G Gray, Siobhan Nicholson, Niamh Leonard, Ronan Ryan, Vincent Young, John J O'Leary, Sinead Cuffe, Stephen P Finn, Kenneth J O'Byrne, Martin P Barr
Non-small cell lung cancer (NSCLC) accounts for a large proportion of cancer deaths and is characterized by low treatment response rates and poor overall prognosis. In the absence of specific treatable mutations, cisplatin-based chemotherapy plays an important role in the treatment of this disease. Unfortunately, the development of resistance has become a major therapeutic challenge in the use of this cytotoxic drug. Elucidating the mechanisms underlying this resistance phenotype, may result in the development of novel agents that enhance sensitivity to cisplatin in lung cancer patients...
September 22, 2017: Oncotarget
https://www.readbyqxmd.com/read/29065820/recent-advances-in-antabuse-disulfiram-the-importance-of-its-metal-binding-ability-to-its-anticancer-activity
#17
Maricela Viola-Rhenals, Kush Rohit Patel, Laura Jaimes-Santamaria, Guojun Wu, Jinbao Liu, Q Ping Dou
Disulfiram (DSF, also called tetraethylthiuram disulphide), a disulfide derivative of N,N-diethyldithiocarbamate (DEDTC), is an antialcoholism drug that is currently being repurposed as a promising anticancer drug. DSF has been investigated in many studies, including in vitro, in vivo, preclinical and clinical. Various mechanisms have been proposed to be responsible for the cytotoxic effect of DSF on cancer cells. DSF is a pro-drug which is converted to its metabolite DEDTC in human body. A complex of DEDTC with a metal ion [usually Cu(II) or Zn(II)] could be responsible for the anticancer activity of DSF in breast, prostate, glioblastoma, lung, melanoma, cervical, colorectal cancers as well as myeloma and leukemia...
October 23, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29029481/cell-cycle-specific-radiosensitisation-by-the-disulfiram-and-copper-complex
#18
Mathias Tesson, Giorgio Anselmi, Caitlin Bell, Robert Mairs
The disulfiram and copper complex (DSF:Cu) has emerged as a potent radiosensitising anti-cancer agent. The ability of copper to stabilise DSF in a planar conformation and to inhibit DNA replication enzymes stimulated our investigation of the effect of DSF:Cu on cell cycle regulation. Flow cytometry and immunoblotting were used to assess the effect of DSF:Cu on cell cycle progression of the neuroblastoma cell line SK-N-BE(2c) and the glioma cell line UVW. Treatment with 0.1 and 0.3 μM DSF:Cu inhibited DNA synthesis in SK-N-BE(2c) and UVW cells, respectively...
September 12, 2017: Oncotarget
https://www.readbyqxmd.com/read/29016275/effectiveness-of-psychoanalytic-interactional-group-therapy-vs-behavioral-group-therapy-in-routine-outpatient-treatment-of-alcohol-dependent-patients
#19
Peter W Nyhuis, Eva Niederhofer, Norbert Scherbaum, Fabrizio Schifano, Udo Bonnet, Nikolai Dembski, Anna Niederhofer, Michael Specka, Meike Tenbergen
BACKGROUND: The cognitive behavioral therapy has been extensively investigated to assess relapse prevention rates in patients with alcohol dependence. In contrast, only little is known regarding the effectiveness of psychoanalytical psychotherapy in relapse prevention, although this treatment is widely used and especially so in Germany. The aim of this quasi-randomized study was to compare the effectiveness of these two group treatments' approaches under the condition of routine outpatient treatment in a non-university hospital...
October 10, 2017: Substance Use & Misuse
https://www.readbyqxmd.com/read/28974447/synergistic-toxicity-of-epigallocatechin-3-gallate-and-diethyldithiocarbamate-a-lethal-encounter-involving-redox-active-copper
#20
Ke Zhang, Ruixia Dong, Kang Sun, Xiaoxiao Wang, Jiajia Wang, Chung S Yang, Jinsong Zhang
Dithiocarbamates (DTC) are widely used in agricultural, industrial and therapeutic domains. There are ample opportunities for human exposure to DTC. Green tea extracts, with epigallocatechin-3-gallate (EGCG) being the most abundant constituent, have been used as dietary supplements for body weight reduction. Our hypothesis is that DTC can act as a copper ionophore to increase hepatic levels of redox-active copper which promotes EGCG auto-oxidation to produce oxidative stress and toxicity. The results of the present study in a mouse model is consistent with this hypothesis, showing that co-administration of EGCG and diethyldithiocarbamate - a metabolite of disulfiram (a drug for alcohol aversion therapy), both at tolerable levels, caused lethality...
September 30, 2017: Free Radical Biology & Medicine
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