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https://www.readbyqxmd.com/read/29908515/an-altered-state-emergent-changes-to-illicit-drug-markets-and-distribution-networks-in-scotland
#1
James Densley, Robert McLean, Ross Deuchar, Simon Harding
BACKGROUND: Many efforts have been undertaken to construct an overview of various aspects of illicit drug distribution in the United Kingdom. Yet given that national, regional, and local differences can be profound, this has proven difficult, to the extent that Scotland has been largely excluded from the conversation. In addition, the level of supply being examined, the drug type, and the actors involved only add to confusion and vast differences between some findings. METHOD: The current study aims to provide a holistic account, as best as possible considering variations of illegal drug supply in illicit networks, by focusing in on a particular geographical context (Scotland) and addressing drug supply at all levels...
June 13, 2018: International Journal on Drug Policy
https://www.readbyqxmd.com/read/29908497/stereoselective-effects-of-ibuprofen-in-adult-zebrafish-danio-rerio-using-uplc-tof-ms-based-metabolomics
#2
Yue Song, Tingting Chai, Zhiqiang Yin, Xining Zhang, Wei Zhang, Yongzhong Qian, Jing Qiu
Ibuprofen (IBU), as a commonly used non-steroidal anti-inflammatory drug (NSAID) and pharmaceutical and personal care product (PPCP), is frequently prescribed by doctors to relieve pain. It is widely released into environmental water and soil in the form of chiral enantiomers by the urination and defecation of humans or animals and by sewage discharge from wastewater treatment plants. This study focused on the alteration of metabolism in the adult zebrafish (Danio rerio) brain after exposure to R-(-)-/S-(+)-/rac-IBU at 5 μg L-1 for 28 days...
June 9, 2018: Environmental Pollution
https://www.readbyqxmd.com/read/29908483/sex-differences-in-nicotine-dependency-and-depressive-tendency-among-smokers
#3
Maki Komiyama, Hajime Yamakage, Noriko Satoh-Asahara, Yuka Ozaki, Tatsuya Morimoto, Akira Shimatsu, Yuko Takahashi, Koji Hasegawa
Depressive tendency and nicotine dependency are factors related to the failure of smoking cessation. Women generally have a higher depressive tendency and difficulty in smoking cessation than men. However, the impact of sex differences on the relationship between nicotine dependency and depressive tendency remains unclear. We evaluated 727 patients (496 men and 231 women) who visited our outpatient clinic for smoking cessation therapy and compared various parameters measured between sexes during consultation...
June 9, 2018: Psychiatry Research
https://www.readbyqxmd.com/read/29908471/searching-for-synergistic-calcium-antagonists-and-novel-therapeutic-regimens-for-coronary-heart-disease-therapy-from-a-traditional-chinese-medicine-suxiao-jiuxin-pill
#4
Wei Lei, Jianan Ni, Xueting Xia, Min Jiang, Gang Bai
Coronary heart disease is a vital cause of morbidity and mortality worldwide, and calcium channel blockers (CCBs) are important drugs that can be used to treat cardiovascular diseases. Suxiao Jiuxin Pill (SX), a traditional Chinese medicine, is widely used as an emergency drug for coronary heart disease therapy. However, understanding its potential mechanism in intracellular calcium concentration ([Ca2+ ]i ) modulation remains a challenge. To identify the active pharmacological ingredients (APIs) and reveal a novel combination therapy for ameliorating cardiovascular diseases, the ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC/Q-TOF MS) combined with a dual-luciferase reporter [Ca2+ ]i assay system was applied...
June 8, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29908468/first-report-on-the-pharmacokinetic-profile-of-nimbolide-a-novel-anticancer-agent-in-oral-and-intravenous-administrated-rats-by-lc-ms-method
#5
Shandilya Mahamuni Baira, Amit Khurana, Jaganmohan Somagoni, R Srinivas, Chandraiah Godugu, M V N Kumar Talluri
Nimbolide is a novel, natural compound with promising potential as a drug candidate for anticancer activity. It is isolated from the Indian traditional medicinal plant Azadirachta indica popularly known as neem. The present study was undertaken to explore the oral bioavailability and pharmacokinetic characteristics of nimbolide in rats using the LC/QTOF/MS method. A simple protein precipitation method using acetonitrile was employed for extracting nimbolide from rat plasma. The chromatographic separation of nimbolide and the internal standard (regorafenib) was attained on an Aquity BEH C18 column (100 × 2...
June 2, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29908451/inhibitors-of-protein-protein-interactions-ppis-an-analysis-of-scaffold-choices-and-buried-surface-area
#6
REVIEW
Xu Ran, Jason E Gestwicki
Protein-protein interactions (PPI) were once considered 'undruggable', but clinical successes, driven by advanced methods in drug discovery, have challenged that notion. Here, we review the last three years of literature on PPI inhibitors to understand what is working and why. From the 66 recently reported PPI inhibitors, we found that the average molecular weight was significantly greater than 500Da, but that this trend was driven, in large part, by the contribution of peptide-based compounds. Despite differences in average molecular weight, we found that compounds based on small molecules or peptides were almost equally likely to be potent inhibitors (KD <1μM)...
June 13, 2018: Current Opinion in Chemical Biology
https://www.readbyqxmd.com/read/29908444/synthesis-and-biological-evaluation-of-novel-2-oxo-1-2-dihydroquinoline-4-carboxamide-derivatives-for-the-treatment-of-esophageal-squamous-cell-carcinoma
#7
Mai I Shahin, Joyeeta Roy, Maha Hanafi, Dongyao Wang, Urarika Luesakul, Yifeng Chai, Nongnuj Muangsin, Deena S Lasheen, Dalal A Abou El Ella, Khaled A Abouzid, Nouri Neamati
No new and effective treatments have been approved for the treatment of esophageal squamous cell carcinoma (ESCC) in the past decade. Cisplatin and 5-fluoruracil are the most commonly used drugs for this disease. In order to develop a new class of drugs effective in our ESCC phenotypic screens, we began a systematic approach to generate novel compounds based on the 2-oxo-1,2-dihydroquinoline-4-carboxamide fragment. Herein, we report on the synthesis and initial assessment of 55 new analogues in two ESCC cell lines...
May 29, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29908443/novel-pyrimidinic-selenourea-induces-dna-damage-cell-cycle-arrest-and-apoptosis-in-human-breast-carcinoma
#8
Flavio A R Barbosa, Tâmila Siminski, Rômulo F S Canto, Gabriela M Almeida, Nádia S R S Mota, Fabiana Ourique, Rozangela Curi Pedrosa, Antonio Luiz Braga
Novel pyrimidinic selenoureas were synthesized and evaluated against tumour and normal cell lines. Among these, the compound named 3j initially showed relevant cytotoxicity and selectivity for tumour cells. Three analogues of 3j were designed and synthesized keeping in view the structural requirements of this compound. Almost all the tested compounds displayed considerable cytotoxicity. However, 8a, one of the 3j analogues, was shown to be highly selective and cytotoxic, especially for breast carcinoma cells (MCF-7) (IC50  = 3...
June 11, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29908442/benzomorphan-skeleton-a-versatile-scaffold-for-different-targets-a-comprehensive-review
#9
REVIEW
Rita Turnaturi, Lucia Montenegro, Agostino Marrazzo, Rosalba Parenti, Lorella Pasquinucci, Carmela Parenti
Despite the fact that the benzomorphan skeleton has mainly been employed in medicinal chemistry for the development of opioid analgesics, it is a versatile structure. Its stereochemistry, as well as opportune modifications at the phenolic hydroxyl group and at the basic nitrogen, play a pivotal role addressing the benzomorphan-based compounds to a specific target. In this review, we describe the structure activity-relationships (SARs) of benzomorphan-based compounds acting at sigma 1 receptor (σ1R), sigma 2 receptor (σ2R), voltage-dependent sodium channel, N-Methyl-d-Aspartate (NMDA) receptor-channel complex and other targets...
June 7, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29908440/organometallic-compounds-in-the-discovery-of-new-agents-against-kinetoplastid-caused-diseases
#10
REVIEW
Mauro Ravera, Elsa Moreno-Viguri, Rocio Paucar, Silvia Pérez-Silanes, Elisabetta Gabano
The development of safe and affordable antiparasitic agents effective against neglected tropical diseases is a big challenge of the drug discovery. The drugs currently employed have limitations such as poor efficacy, drug resistance or side effects. Thus, the search for new promising drugs is more and more crucial. Metal complexes and, in particular, organometallic compounds may expand the list of the drug candidates due to the peculiar attributes that the presence of the metal core add to the organic fragment (e...
June 1, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29908438/targeting-rna-polymerase-i-transcription-machinery-in-cancer-cells-by-a-novel-monofunctional-platinum-based-agent
#11
Zhen-Lei Zhang, Chun-Lai Zhao, Qian Chen, Kai Xu, Xin Qiao, Jing-Yuan Xu
Aberrant ribosome biogenesis and enlarged nucleoli have long been used by pathologists as a marker of aggressive tumors. Suppression of RNA polymerase I (Pol I) transcription machinery within the nucleolus could be a direct way to trigger the nucleolar stress and to inhibit the rapid proliferation of cancer cells. Here we modified cisplatin with an analogue of the selective inhibitor of RNA polymerase I-mediated transcription BMH-21 to develop a novel platinum-based Pol I selective inhibitor. We show that this novel monofunctional platinum-based agent, P1-B1, had enhanced antitumor activity of up to 17-fold greater than the clinical drug cisplatin in cisplatin-resistant non-small cell lung cancer cells...
June 1, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29908424/high-dispersed-phyto-phospholipid-complex-tpgs-1000-with-mesoporous-silica-to-enhance-oral-bioavailability-of-tanshinol
#12
Mengmeng Yang, Ting Chen, Lingchong Wang, Lihua Chen, Junsong Li, Liuqing Di
Phenolic acids are widely distributed in the plant kingdom and possess a broad spectrum of pharmacological activity. However, low oral bioavailability restricts their application. In this study, a high dispersed phyto- phospholipid complex with mesoporous silica containing TPGS 1000 (TPC-SD) was fabricated using Tanshinol (Tan) as model drug. Phospholipid complex (PC) was employed to improve the n-octanol/water partition coefficient (log P) and apparent permeability coefficients (Papp ) of Tan. Mesoporous silica was used to compensate for the negative effects of phospholipid on drug's dispersion and dissolution owing to its viscosity and poor water-solubility...
June 9, 2018: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29908386/anxiety-is-common-and-independently-associated-with-clinical-features-of-epilepsy
#13
Heidi M Munger Clary, Beverly M Snively, Marla J Hamberger
OBJECTIVE: The objective of this study was to assess for independent association of anxiety symptoms with epilepsy localization and other epilepsy-related and demographic factors in a large tertiary care adult epilepsy population. METHODS: Among 540 adults, anxiety was measured by the Symptom Checklist 90-R (SCL-90R) anxiety subscale, and detailed demographics, epilepsy localization, and depression scores (SCL-90R) were collected. High anxiety was defined by SCL-90R anxiety T-score ≥ 60...
June 13, 2018: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/29908359/statin-therapy-does-not-reduce-liver-fat-scores-in-patients-receiving-antiretroviral-therapy-for-hiv-infection
#14
Vanessa El Kamari, Corrilynn O Hileman, Pierre M Gholam, Manjusha Kulkarni, Nicholas Funderburg, Grace A McComsey
BACKGROUND & AIMS: Therapies are needed to limit progression of fatty liver diseases in patients with HIV infection. We analyzed data from a prospective study of the effects of rosuvastatin (a statin) on hepatic steatosis in HIV-positive adults. METHODS: We performed secondary analysis of data from a double-blind trial of adult patients with HIV infection (78% male; 68% African American; mean age, 46 years; body mass index, 29 kg/m2 ; HIV1 RNA<1000 copies/mL; LDL-cholesterol <130 mg/dL) receiving antiretroviral therapy...
June 13, 2018: Clinical Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/29908354/optimal-timing-for-elective-total-hip-replacement-in-hiv-positive-patients
#15
Chun-Hung Chang, Shang-Wen Tsai, Cheng-Fong Chen, Po-Kuei Wu, Wing-Wai Wong, Ming-Chau Chang, Wei-Ming Chen
INTRODUCTION: Evidence about the optimal timing for total hip replacement (THR) in HIV-positive patients is scant. HYPOTHESIS: Preoperative criteria: cluster of differentiation 4 (CD4) counts>200 cells/mm3 and an undetectable HIV virus load before THR, improve infection rates, aseptic loosenings, and functional outcomes. MATERIALS AND METHODS: We recruited 16 HIV-positive patients who had undergone 25 THRs between 2003 and 2015. None had hemophilia, and none were intravenous drug users (IVDUs)...
June 13, 2018: Orthopaedics & Traumatology, Surgery & Research: OTSR
https://www.readbyqxmd.com/read/29908336/positive-reinforcement-targeting-abstinence-in-substance-misuse-praise-study-protocol-for-a-cluster-rct-process-evaluation-of-contingency-management
#16
N Metrebian, T Weaver, S Pilling, J Hellier, S Byford, J Shearer, L Mitcheson, M Astbury, P Bijral, N Bogdan, O Bowden-Jones, E Day, J Dunn, E Finch, S Forshall, A Glasper, G Morse, S Akhtar, J Bajaria, C Bennett, E Bishop, V Charles, C Davey, R Desai, C Goodfellow, F Haque, N Little, H McKechnie, J Morris, F Mosler, J Mutz, R Pauli, D Poovendran, E Slater, J Strang
There are approximately 256,000 heroin and other opiate users in England of whom 155,000 are in treatment for heroin (or opiate) addiction. The majority of people in treatment receive opiate substitution treatment (OST) (methadone and buprenorphine). However, OST suffers from high attrition and persistent heroin use even whilst in treatment. Contingency management (CM) is a psychological intervention based on the principles of operant conditioning. It is delivered as an adjunct to existing evidence based treatments to amplify patient benefit and involves the systematic application of positive reinforcement (financial or material incentives) to promote behaviours consistent with treatment goals...
June 13, 2018: Contemporary Clinical Trials
https://www.readbyqxmd.com/read/29908332/enhanced-nanoparticle-uptake-into-virus-infected-cells-could-nanoparticles-be-useful-in-antiviral-therapy
#17
Yasmin Abo-Zeid, Richard A Urbanowicz, Brian J Thomson, William L Irving, Alexander W Tarr, Martin C Garnett
Virus infections cause diseases of different severity ranged from mild infection e.g. common cold into life threating diseases e.g. Human Immunodeficiency virus (HIV), Hepatitis B. Virus infections represent 44% of newly emerging infections. Although there are many efficient antiviral agents, they still have drawbacks due to accumulation at off target organs and developing of virus resistance due to virus mutation. Therefore, developing a delivery system that can selectively target drug into affected organs and avoid off target accumulation would be a highly advantageous strategy to improve antiviral therapy...
June 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29908331/all-atomistic-molecular-dynamics-aa-md-studies-and-pharmacokinetic-performance-of-pamam-dendrimer-furosemide-delivery-systems
#18
Daniel P Otto, Melgardt M de Villiers
Improvement of problematic dissolution and solubility properties of a model drug, furosemide, was investigated for poly(amidoamine) (PAMAM) dendrimer complexes of the drug. Full and half generation dendrimers with amino and ester terminals respectively, were studied. In vitro release performance of these complexes was investigated at drug loads ranging 5-60% using simulated gastric fluids. Full generation dendrimers accommodated higher drug loads, outperformed half-generation complexes, and free drug. Pharmacokinetic studies in rats indicated that the dendrimer complexes markedly improved in the bioavailability of the drug compared to the unformulated drug...
June 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29908330/a-preliminary-study-for-the-development-and-optimization-by-experimental-design-of-an-in-vitro-method-for-prediction-of-drug-buccal-absorption
#19
Paola Mura, Serena Orlandini, Marzia Cirri, Francesca Maestrelli, Natascia Mennini, Giada Casella, Sandra Furlanetto
The work was aimed at developing an in vitro method able to provide rapid and reliable evaluation of drug absorption through buccal mucosa. Absorption simulator apparatus endowed with an artificial membrane was purposely developed by experimental design. The apparent permeation coefficient (Papp ) through excised porcine buccal mucosa of naproxen, selected as model drug, was the target value to obtain with the artificial membrane. The multivariate approach enabled systematic evaluation of the effect on the response (Papp ) of simultaneous variations of the variables (kind of lipid components for support impregnation and relative amounts)...
June 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29908320/exploring-the-multi-drug-resistance-in-escherichia-coli-o157-h7-by-gene-interaction-network-a-systems-biology-approach
#20
Sravan Kumar Miryala, Sudha Ramaiah
In the present study, we have constructed an interaction network of 29 antibiotic resistant genes along with 777 interactions in E. coli O157:H7. Gene ontology analysis reveals that 94, 89 and 67 genes have roles in the cellular process, biological process and molecular function respectively. Gene complexes related to tripartite efflux pumps mdtEF-tolC and ABC family efflux pump macAB-tolC play key roles in multidrug efflux systems. It is noteworthy to mention that, 19 genes are involved in multi-efflux pumps and they play a significant role in multidrug resistance (MDR); while 18 genes are vital for fatty acid synthesis...
June 13, 2018: Genomics
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