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https://www.readbyqxmd.com/read/29778006/environmentally-relevant-concentrations-of-tramadol-and-citalopram-alter-behaviour-of-an-aquatic-invertebrate
#1
M Buřič, K Grabicová, J Kubec, A Kouba, I Kuklina, P Kozák, R Grabic, T Randák
Environmental pollution by pharmaceutically active compounds, used in quantities similar to those of pesticides and other organic micropollutants, is increasingly recognized as a major threat to the aquatic environment. These compounds are only partly removed from wastewaters and, despite their low concentrations, directly and indirectly affect behaviour of freshwater organisms in natural habitats. The aim of this study was to behaviourally assess the effects of an opioid painkiller (tramadol) and antidepressant drug (citalopram) on behaviour patterns of a clonal model species, marbled crayfish...
May 14, 2018: Aquatic Toxicology
https://www.readbyqxmd.com/read/29777957/dual-ph-reduction-responsive-hybrid-polymeric-micelles-for-targeted-chemo-photothermal-combination-therapy
#2
Linhua Zhang, Yu Qin, Zhiming Zhang, Fan Fan, Chenlu Huang, Li Lu, Hai Wang, Xu Jin, Hanxue Zhao, Deling Kong, Chun Wang, Hongfan Sun, Xigang Leng, Dunwan Zhu
The combination of chemotherapy and photothermal therapy in multifunctional nanovesicles has emerged as a promising strategy to improve cancer therapeutic efficacy. Herein, we designed new pH/reduction dual-responsive and folate decorated polymeric micelles (FA Co-PMs) as theranostic nanocarrier to co-encapsulate doxorubicin (DOX) and indocyanine green (ICG) for targeted NIR imaging and chemo-photothermal combination therapy. The Co-PMs exhibited nano-sized structure (∼100 nm) with good monodispersity, high encapsulation efficiency of both ICG and DOX, triggered DOX release in response to acid pH and reduction environment, and excellent temperature conversion with laser irradiation...
May 16, 2018: Acta Biomaterialia
https://www.readbyqxmd.com/read/29777955/perspectives-and-limitations-for-nucleo-t-side-analogs-in-future-hbv-therapies
#3
REVIEW
Massimo Levrero, Miroslava Subic, Francois Villeret, Fabien Zoulim
The latest generation of nucleo(t)side analogs (NAs) provide robust virus suppression with high barrier to resistance. Long term NAs treatment is associated with a partial restoration in HBV-specific T-cell functions, regression of fibrosis, no disease progression and a reduction of HCC risk but rarely lead to cure and life-long treatments is often required. New insights into the hepatitis B viral life cycle and the host immune response have expanded the potential targets for drug therapies with interesting antiviral candidates and novel immunotherapeutic approaches in early stage development...
May 16, 2018: Current Opinion in Virology
https://www.readbyqxmd.com/read/29777923/diagnosis-and-management-of-pulmonary-infection-due-to-rhodococcus-equi
#4
REVIEW
Weijie V Lin, Robert L Kruse, Katharine Yang, Daniel M Musher
BACKGROUND: Rhodococcus equi is a recognized cause of disease in humans, especially in patients who are immunocompromised. Because diphtheroids are regarded as part of normal respiratory flora, the importance of R. equi as a pulmonary pathogen may not be fully appreciated and its prevalence underestimated. Most treatment recommendations for R. equi infection were established before antiretroviral drugs became available for HIV/AIDS therapy, and therapeutic strategies may need to be updated...
May 16, 2018: Clinical Microbiology and Infection
https://www.readbyqxmd.com/read/29777871/pain-therapeutics-from-cone-snail-venoms-from-ziconotide-to-novel-non-opioid-pathways
#5
Helena Safavi-Hemami, Shane E Brogan, Baldomero M Olivera
There have been numerous attempts to develop non-opioid drugs for severe pain, but the vast majority of these efforts have failed. A notable exception is Ziconotide (Prialt®), approved by the FDA in 2004. In this review, we summarize the present status of Ziconotide as a therapeutic drug and introduce a wider framework: the potential of venom peptides from cone snails as a resource providing a continuous pipeline for the discovery of non-opioid pain therapeutics. An auxiliary theme that we hope to develop is that these venoms, already a validated starting point for non-opioid drug leads, should also provide an opportunity for identifying novel molecular targets for future pain drugs...
May 16, 2018: Journal of Proteomics
https://www.readbyqxmd.com/read/29777855/polymer-lipid-hybrid-nanoparticles-as-enhanced-indomethacin-delivery-systems
#6
Annalisa Dalmoro, Sabrina Bochicchio, Shamil F Nasibullin, Paolo Bertoncin, Gaetano Lamberti, Anna Angela Barba, Rouslan I Moustafine
Non-steroidal anti-inflammatory drugs (NSAIDs), i.e. indomethacin used for rheumatoid arthritis and non-rheumatoid inflammatory diseases, are known for their injurious actions on the gastrointestinal (GI) tract. Mucosal damage can be avoided by using nanoscale systems composed by a combination of liposomes and biodegradable natural polymer, i.e. chitosan, for enhancing drug activity. Aim of this study was to prepare chitosan-lipid hybrid delivery systems for indomethacin dosage through a novel continuous method based on microfluidic principles...
May 16, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29777797/polypharmacy-defined-as-taking-five-or-more-drugs-is-inadequate-in-the-cardiovascular-setting
#7
Nazanin Abolhassani
BACKGROUND: By how much polypharmacy (defined by number of drugss) differs from polyactive ingredient use (defined by the number of pharmacologically active ingredients) has not been assessed. OBJECTIVES: to compare the extent of polypharmacy vs. polyactive ingredients among patients taking CV medicines. METHODS: Prospective, 10-year follow-up study conducted among 880 participants of the CoLaus study taking CV drugs at baseline. Polypharmacy was defined as the use of 5 or more CV medicines; polyactive ingredient use was defined as the use of 5 or more pharmacologically active CV ingredients...
May 16, 2018: Journal of Clinical Epidemiology
https://www.readbyqxmd.com/read/29777795/sirna-in-ovarian-cancer-delivery-strategies-and-targets-for-therapy
#8
REVIEW
Dirk van den Brand, Vicky Mertens, Leon F A G Massuger, Roland Brock
Epithelial ovarian cancer (EOC) is the most lethal gynecological malignancy, and the sixth leading cause of cancer related death in women overall. Despite improved surgical techniques and advances in chemotherapy, mortality hardly decreased over the last twenty years. The major problem is that (micro)metastases persevere in the abdominal cavity, causing incurable tumor recurrence. Therefore, there is an imminent need for new therapeutic strategies. Oligonucleotide (ON) based therapies such as RNA interference (RNAi) provide the possibility to specifically address disease-related pathways...
May 16, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29777794/regulatory-t-cell-targeted-hybrid-nanoparticles-combined-with-immuno-checkpoint-blockage-for-cancer-immunotherapy
#9
Wenquan Ou, Raj Kumar Thapa, Liyuan Jiang, Soe Zar Chi, Milan Gautam, Jae-Hoon Chang, Jee-Heon Jeong, Sae Kwang Ku, Han-Gon Choi, Chul Soon Yong, Jong Oh Kim
Immunosuppression in tumor microenvironments induced by regulatory T (Treg) cells is regarded a critical mechanism of tumor immune escape and poses a major impediment to cancer immunotherapy. In this study, we developed tLyp1 peptide-conjugated hybrid nanoparticles for targeting Treg cells in the tumor microenvironment. The tLyp1 peptide-modified hybrid nanoparticles presented good stability and effective targeting to Treg cells, and they enhanced the effect of imatinib in downregulating Treg cell suppression through inhibition of STAT3 and STAT5 phosphorylation...
May 16, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29777783/accelerated-lipid-catabolism-and-autophagy-are-cancer-survival-mechanisms-under-inhibited-glutaminolysis
#10
Anna Halama, Michal Kulinski, Shaima S Dib, Shaza B Zaghlool, Kodappully S Siveen, Ahmad Iskandarani, Jonas Zierer, Kirti S Prabhu, Noothan J Satheesh, Aditya M Bhagwat, Shahab Uddin, Gabi Kastenmüller, Olivier Elemento, Steven S Gross, Karsten Suhre
Suppressing glutaminolysis does not always induce cancer cell death in glutamine dependent tumors because cells may switch to alternative energy sources. To reveal compensatory metabolic pathways, we investigated the metabolome-wide cellular response to inhibited glutaminolysis in cancer cells. Glutaminolysis inhibition with C.968 suppressed cell proliferation but was insufficient to induce cancer cell death. We found that lipid catabolism was activated as a compensation for glutaminolysis inhibition. Accelerated lipid catabolism, together with oxidative stress induced by glutaminolysis inhibition, triggered autophagy...
May 16, 2018: Cancer Letters
https://www.readbyqxmd.com/read/29777772/improving-maraviroc-oral-bioavailability-by-formation-of-solid-drug-nanoparticles
#11
Alison C Savage, Lee M Tatham, Marco Siccardi, Trevor Scott, Manoli Vourvahis, Andrew Clark, Steve P Rannard, Andrew Owen
Oral drug administration remains the preferred approach for treatment of HIV in most patients. Maraviroc (MVC) is the first in class co-receptor antagonist, which blocks HIV entry into host cells. MVC has an oral bioavailability of approximately 33%, which is limited by poor permeability as well as affinity for CYP3A and several drug transporters. While once-daily doses are now the favoured option for HIV therapy, dose-limiting postural hypotension has been of theoretical concern when administering doses high enough to achieve this for MVC (particularly during coadministration of enzyme inhibitors)...
May 16, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/29777719/purification-and-identification-of-an-actinomycin-d-analogue-from-actinomycetes-associated-with-ganoderma-applanatum-via-magnetic-molecularly-imprinted-polymers-and-tandem-mass-spectrometry
#12
Chang-Gen Li, Bo Yuan, Meng-Meng Dong, Pin-Yu Zhou, Yu-Xin Hao, Ying-Ying Sun, Meng-Ke Xu, Dan Li, Guo-Yin Kai, Ji-Hong Jiang
Actinomycetes are main producers of antibiotics and targeted screening could improve the efficiency of discovering new drugs. This study describes, for the first time, the isolation of endophytic actinomycetes from the macrofungus Ganoderma applanatum. To increase the efficiency of screening, novel actinomycin D (Act D) molecularly-imprinted polymers were adsorbed to the surface of Fe3 O4 @SiO2 magnetic microspheres (MMIPs) and using in the isolation. A monolithic column prepared with magnetic molecularly imprinted polymers was employed to adsorb actinomycin D and its analogues for selective analysis and identification via MS/MS spectroscopy...
May 16, 2018: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/29777519/combination-glucose-lowering-therapy-plans-in-t2dm-case-based-considerations
#13
REVIEW
Lawrence Blonde, Susana Dipp, Daniel Cadena
Type 2 diabetes mellitus (T2DM) is a complex disease, and while lifestyle interventions remain the cornerstone of therapy, most patients will also require pharmacotherapy. Current diabetes treatment guidelines and algorithms recommend an individualized approach to setting glycemic goals and selecting treatment. Although a single antihyperglycemic agent may be appropriate as the initial T2DM pharmacotherapy, the progressive nature of the disease due to declining pancreatic β-cell function will result in the vast majority of T2DM patients eventually requiring two or more antihyperglycemic agents...
May 18, 2018: Advances in Therapy
https://www.readbyqxmd.com/read/29777495/ameliorative-effect-of-ginseng-extract-on-phthalate-and-bisphenol-a-reprotoxicity-during-pregnancy-in-rats
#14
Islam M Saadeldin, Mohamed A Hussein, Aida Hamid Suleiman, Mahmoud G Abohassan, Mona M Ahmed, Amr A Moustafa, Abdullah F Moumen, Ayman Abdel-Aziz Swelum
Phthalates (such as DEHP) and bisphenol A (BPA) are widely used chemicals in plastics manufacturing and exert public health concerns as endocrine disrupters. This study was designed to investigate the deleterious effect of DEHP and BPA on endocrine profile of pregnant female rats and the combined treatment with ginseng extract (Panax ginseng). Seventy-two pregnant rats were divided into six groups (control, ginseng, DEHP, BPA, Gin + DEHP, and Gin + BPA), 12 females per each group. The drugs were supplemented from pregnancy day 0 until day 20...
May 18, 2018: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/29777433/are-pcsk9-inhibitors-cost-effective
#15
Max J Korman, Kjetil Retterstøl, Ivar Sønbø Kristiansen, Torbjørn Wisløff
The objective of this study was to review available health economic evaluations of PCSK9 (proprotein convertase subtilisin/kexin type 9) inhibitors. These drugs reduce low-density lipid cholesterol levels and cardiovascular risk, but their cost effectiveness has been questioned. We searched Medline and Embase for economic evaluations in any language at any time. Studies were included if they analysed any PCSK9 inhibitor compared with either statin alone or in combination with ezetimibe or any other therapy considered standard prior to the introduction of PCSK9 inhibitors...
May 18, 2018: PharmacoEconomics
https://www.readbyqxmd.com/read/29777431/modified-anterior-palatoplasty-and-double-suspension-sutures-with-or-without-tonsillectomy-in-selected-patients-with-obstructive-sleep-apnea-a-preliminary-report
#16
Sherif M Askar, Mohammad W El-Anwar, Ali Awad
BACKGROUND: Retropalatal region might be considered the most common site of obstruction in patients with snoring and OSA. We aimed at presentation of two combined techniques: modified anterior palatoplasty (MAP) and bilateral double suspension suture (DSS). METHODS: This prospective study was conducted on OSA patients with retro-palatal collapse only that was confirmed by nasoendoscopy during Muller's maneuver and drug induced sleep endoscopy. MAP and DSS were performed for all patients...
May 18, 2018: Sleep & Breathing, Schlaf & Atmung
https://www.readbyqxmd.com/read/29777407/modelling-the-delay-between-pharmacokinetics-and-eeg-effects-of-morphine-in-rats-binding-kinetic-versus-effect-compartment-models
#17
Wilhelmus E A de Witte, Vivi Rottschäfer, Meindert Danhof, Piet H van der Graaf, Lambertus A Peletier, Elizabeth C M de Lange
Drug-target binding kinetics (as determined by association and dissociation rate constants, k on and k off ) can be an important determinant of the kinetics of drug action. However, the effect compartment model is used most frequently instead of a target binding model to describe hysteresis. Here we investigate when the drug-target binding model should be used in lieu of the effect compartment model. The utility of the effect compartment (EC), the target binding kinetics (TB) and the combined effect compartment-target binding kinetics (EC-TB) model were tested on either plasma (ECPL , TBPL and EC-TBPL ) or brain extracellular fluid (ECF) (ECECF , TBECF and EC-TBECF ) morphine concentrations and EEG amplitude in rats...
May 18, 2018: Journal of Pharmacokinetics and Pharmacodynamics
https://www.readbyqxmd.com/read/29777389/iron-based-metal-organic-frameworks-as-a-theranostic-carrier-for-local-tuberculosis-therapy
#18
Gabriela Wyszogrodzka, Przemysław Dorożyński, Barbara Gil, Wieslaw J Roth, Maciej Strzempek, Bartosz Marszałek, Władysław P Węglarz, Elżbieta Menaszek, Weronika Strzempek, Piotr Kulinowski
PURPOSE: The purpose of the study was initial evaluation of applicability of metal organic framework (MOF) Fe-MIL-101-NH2 as a theranostic carrier of antituberculous drug in terms of its functionality, i.e. drug loading, drug dissolution, magnetic resonance imaging (MRI) contrast and cytotoxic safety. METHODS: Fe-MIL-101-NH2 was characterized using X-ray powder diffraction, FTIR spectrometry and scanning electron microscopy. The particle size analysis was determined using laser diffraction...
May 18, 2018: Pharmaceutical Research
https://www.readbyqxmd.com/read/29777330/down-regulating-il-6-gp130-targets-improved-the-anti-tumor-effects-of-5-fluorouracil-in-colon-cancer
#19
Sanhong Li, Jilai Tian, Hongming Zhang, Shoubing Zhou, Xiyong Wang, Lei Zhang, Jiapeng Yang, Zhigang Zhang, Zhenling Ji
Recent studies have confirmed that IL-6/GP130 targets are closely associated with tumor growth, metastasis and drug resistance. 5-Fluorouracil (5-FU) is the most common chemotherapeutic agent for colon cancer but is limited due to chemoresistance and high cytotoxicity. Bazedoxifene (BZA), a third-generation selective estrogen receptor modulator, was discovered by multiple ligand simultaneous docking and drug repositioning approaches to have a novel function as an IL-6/GP130 target inhibitor. Thus, we speculated that in colon cancer, the anti-tumor efficacy of 5-FU might be increased in combination with IL-6/GP130 inhibitors...
May 18, 2018: Apoptosis: An International Journal on Programmed Cell Death
https://www.readbyqxmd.com/read/29777203/ginkgo-biloba-extracts-prevent-aortic-rupture-in-angiotensin-ii-infused-hypercholesterolemic-mice
#20
Xiao-Fang Huang, Song-Zhao Zhang, Ya-Yu You, Na Zhang, Hong Lu, Alan Daugherty, Xiao-Jie Xie
Abdominal aortic aneurysms (AAAs) are a chronic vascular disease characterized by pathological luminal dilation. Aortic rupture is the fatal consequence of AAAs. Ginkgo biloba extracts (GBEs), a natural herb extract widely used as food supplements, drugs, and cosmetics, has been reported to suppress development of calcium chloride-induced AAAs in mice. Calcium chloride-induced AAAs do not rupture, while angiotensin II (AngII)-induced AAAs in mice have high rate of aortic rupture, implicating potentially different mechanisms from calcium chloride-induced AAAs...
May 18, 2018: Acta Pharmacologica Sinica
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