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https://www.readbyqxmd.com/read/29353398/new-strategies-of-arv-the-road-to-simplification
#1
REVIEW
Rosa de Miguel Buckley, Rocio Montejano, Natalia Stella-Ascariz, Jose R Arribas
PURPOSE OF REVIEW: Simplification of antiretroviral therapy is a strategy aiming to reduce pill burden, drug interactions, and toxicity. This review focuses on the most recent and important studies evaluating a reduction on the number of drugs for HIV treatment, both in naive and virologically suppressed patients. RECENT FINDINGS: Interesting studies have been performed in the past years testing dual therapy and monotherapy, with variable rates of virological control...
January 20, 2018: Current HIV/AIDS Reports
https://www.readbyqxmd.com/read/29353288/quercetin-inhibits-breast-cancer-stem-cells-via-downregulation-of-aldehyde-dehydrogenase-1a1-aldh1a1-chemokine-receptor-type-4-cxcr4-mucin-1-muc1-and-epithelial-cell-adhesion-molecule-epcam
#2
Rong Wang, Laixiu Yang, Shen Li, Dongmei Ye, Lihong Yang, Qingyan Liu, Zibo Zhao, Qing Cai, Junzhen Tan, Xiuli Li
BACKGROUND Quercetin, nature's most common flavonoid, possesses anticarcinogenic properties against various forms of cancer. The aim of this study was to investigate the effect of quercetin on breast cancer stem cells in the MDA-MB-231 cell line, and to elucidate the possible mechanisms for those effects. MATERIAL AND METHODS We evaluated breast cancer stem cell proliferation, clone generation, and mammosphere formation to determine the effect of quercetin treatment on breast cancer stem cells. RESULTS In our study, quercetin suppressed breast cancer stem cell proliferation, self-renewal, and invasiveness...
January 21, 2018: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/29353278/stereoselective-inhibition-of-renal-basolateral-human-organic-anion-transporter-3-by-lansoprazole-enantiomers
#3
Yugo Hamada, Kenji Ikemura, Takuya Iwamoto, Masahiro Okuda
Lansoprazole, a proton pump inhibitor, potently inhibits human organic anion transporter, hOAT3 (SLC22A8). Lansoprazole has an asymmetric atom in its structure and is clinically administered as a racemic mixture of (R)-and (S)-enantiomers. However, little is known about the stereoselective inhibitory potencies of lansoprazole against hOAT3 and its homolog, hOAT1. In the present study, the stereoselective inhibitory effect of lansoprazole was evaluated using hOAT1-and hOAT3-expressing cultured cells. hOAT1 and hOAT3 transported [14C]p-aminohippurate and [3H]estrone-3-sulfate (ES) with Michaelis-Menten constants of 29...
January 19, 2018: Pharmacology
https://www.readbyqxmd.com/read/29353039/cetylpyridinium-chloride-as-a-novel-inhibitor-of-hepatitis-b-viral-capsid-assembly
#4
Hyun Wook Seo, Joon Pyung Seo, Yoon Jun Kim, Guhung Jung
Hepatitis B virus (HBV) infection is a major risk factor for chronic liver disease, cirrhosis, and hepatocellular carcinoma (HCC) worldwide. While multiple hepatitis B drugs have been developed, development of drug resistance during treatment or weak efficacies observed in some cases have limited their application. Therefore, there is an urgent need to develop better pharmacological agents for HBV-infected individuals. Here, we identified cetylpyridinium chloride (CPC) as a novel inhibitor of HBV. Using computational analysis of CPC-nucleocapsid proteins, microscale thermophoresis analysis of CPC binding to viral nucleocapsids, and in vitro nucleocapsid formation assays, we found that CPC interacts with dimeric viral nucleocapsid protein (known as core protein or HBcAg)...
January 15, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29352947/novel-organic-inorganic-hybrid-flower-like-structure-of-selenium-nanoparticles-stabilized-by-pullulan-derivatives
#5
Punnida Nonsuwan, Songchan Puthong, Tanapat Palaga, Nongnuj Muangsin
We proudly present the first organic/inorganic hybrid pullulan/SeNPs hybrid microflower material obtained using a simple and bio-inspired strategy. The chemical structures of pullulan, folic acid decorated cationic pullulan (FA-CP) were designed for stabilizing selenium nanoparticles (SeNPs). SeNPs stabilized by FA-CP hybrid microflowers were observed after the addition of a cysteine hydrochloride solution into the solution mixture of Na2SeO3 and FA-CP. We suggested that the concentrations of cysteine and FA-CP were the key factors for the formation of flower-like structure...
March 15, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29352929/structural-characterization-antioxidant-and-hepatoprotective-activities-of-polysaccharides-from-sophorae-tonkinensis-radix
#6
Liangliang Cai, Shanshan Zou, Dengpan Liang, Libiao Luan
In current study we present two polysaccharides, STRP1 and STRP2, purified from Sophorae tonkinensis Radix via column chromatography. Structural analyses indicated that STRP1 and STRP2 were consisted of mannose, rhamnose, glucuronic acid, glucose, galactose and arabinose in a similar molar ratio with main backbones of (1 → 3)-linked-α-d-Gal and (1 → 4)-linked-α-d-Glc, while average molecular weights were 1.30 × 104 and 1.98 × 105 Da, respectively. We observed a strong chelating ability on ferrous ions; substantial radical scavenging activities on DPPH, hydroxyl and superoxide anion radicals in vitro; and significant attenuation on acetaminophen-induced hepatic oxidative damage in mice for STRP1 and STRP2...
March 15, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29352912/synthesis-of-a-poly-ester-dendritic-%C3%AE-cyclodextrin-derivative-by-click-chemistry-combining-the-best-of-two-worlds-for-complexation-enhancement
#7
Luis José López-Méndez, Israel González-Méndez, Rodrigo Aguayo-Ortiz, Laura Dominguez, Sofía L Alcaraz-Estrada, Yareli Rojas-Aguirre, Patricia Guadarrama
In spite of the progress in the cyclodextrins chemistry, the synthesis of monodisperse derivatives with a defined degree of substitution is still a challenge. In this work we present a novel dendritic material produced by combining βCD and second generation poly(ester) dendrons. The selective attachment of dendrons in the seven positions of the βCD-primary face was performed through a CuAAC click reaction, which along with a very simple work-up, allowed obtaining the monodisperse material in very high yields...
March 15, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29352895/sequencing-the-oligosaccharide-pool-in-the-low-molecular-weight-heparin-dalteparin-with-offline-hplc-and-esi-ms-ms
#8
Zhangjie Wang, Tianji Zhang, Shaoshuai Xie, Xinyue Liu, Hongmei Li, Robert J Linhardt, Lianli Chi
Low molecular weight heparins (LMWHs) are widely used anticoagulant drugs. The composition and sequence of LMWH oligosaccharides determine their safety and efficacy. The short oligosaccharide pool in LMWHs undergoes more depolymerization reactions than the longer chains and is the most sensitive indicator of the manufacturing process. Electrospray ionization tandem mass spectrometry (ESI-MS/MS) has been demonstrated as a powerful tool to sequence synthetic heparin oligosaccharide but never been applied to analyze complicated mixture like LMWHs...
March 1, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29352871/a-novel-approach-for-fabricating-nanocomposite-materials-by-embedding-stabilized-core-shell-micelles-into-polysaccharide-cryogel-matrix
#9
Viktoria Pencheva, Elena Margaritova, Maria Borinarova, Marta Slavkova, Denitsa Momekova, Petar D Petrov
We report a novel approach for fabricating nanocomposite polysaccharide-based carriers for sustained delivery of poorly-water-soluble drugs by embedding stabilized core-shell micelles (SPM) possessing hydrophobic cores into super-macroporous hydroxypropyl cellulose (HPC) cryogels. Firstly, nano-sized SPM were synthesized by loading and photochemical crosslinking of pentaerythritoltetraacrylate (PETA) in poly(ethylene oxide)-b-poly(propylene oxide)-b-poly(ethylene oxide) (PEO19PPO29PEO19) core-shell micelles...
March 1, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29352742/cambogin-suppresses-dextran-sulphate-sodium-induced-colitis-by-enhancing-treg-cell-stability-and-function
#10
Yue Lu, Na-Mi Kim, Yi-Wen Jiang, Hong Zhang, Dan Zheng, Fu-Xiang Zhu, Rui Liang, Bin Li, Hong-Xi Xu
BACKGROUND AND PURPOSE: Inflammatory bowel disease (IBD) is a chronic and relapsing inflammatory disorder of gastrointestinal tract, and the dysfunction of immune regulation plays a critical role in IBD. Reflecting the limited use of current drugs and therapies for IBD treatment, it is necessary to explore novel drugs or therapies for this disease. We investigated the effect of cambogin in a mouse model of dextran sulphate sodium (DSS)-induced colitis and whether cambogin attenuates inflammation via Treg-cell-mediated immune modulation...
January 20, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29352713/clinical-variables-associated-with-overall-survival-in-metastatic-castration-resistant-prostate-cancer-patients-treated-with-sipuleucel-t-immunotherapy
#11
Xiao X Wei, Jaselle Perry, Emily Chang, Li Zhang, Robert A Hiatt, Charles J Ryan, Eric J Small, Lawrence Fong
BACKGROUND: Sipuleucel-T is an autologous cell-based cancer immunotherapy for men with asymptomatic or minimally symptomatic metastatic castration-resistant prostate cancer (mCRPC). Its approval by the Food and Drug Administration was based on demonstration of an overall survival (OS) benefit in randomized placebo-controlled phase III trials. However, treatment was associated with a prostate-specific antigen (PSA) decline in only a small minority of patients. Understanding the clinical factors that are associated with OS could help guide treatment decisions, including patient selection and the timing of sipuleucel-T relative to other therapies...
December 27, 2017: Clinical Genitourinary Cancer
https://www.readbyqxmd.com/read/29352704/treatment-of-adult-chronic-indeterminate-chagas-disease-with-benznidazole-and-three-e1224-dosing-regimens-a-proof-of-concept-randomised-placebo-controlled-trial
#12
Faustino Torrico, Joaquim Gascon, Lourdes Ortiz, Cristina Alonso-Vega, María-Jesús Pinazo, Alejandro Schijman, Igor C Almeida, Fabiana Alves, Nathalie Strub-Wourgaft, Isabela Ribeiro
BACKGROUND: Chagas disease is a major neglected vector-borne disease. In this study, we investigated the safety and efficacy of three oral E1224 (a water-soluble ravuconazole prodrug) regimens and benznidazole versus placebo in adult chronic indeterminate Chagas disease. METHOD: In this proof-of-concept, double-blind, randomised phase 2 clinical trial, we recruited adults (18-50 years) with confirmed diagnosis of Trypanosoma cruzi infection from two outpatient units in Bolivia...
January 15, 2018: Lancet Infectious Diseases
https://www.readbyqxmd.com/read/29352387/current-perspectives-on-erythema-multiforme
#13
REVIEW
Marianne Lerch, Carlo Mainetti, Benedetta Terziroli Beretta-Piccoli, Thomas Harr
Recognition and timely adequate treatment of erythema multiforme remain a major challenge. In this review, current diagnostic guidelines, potential pitfalls, and modern/novel treatment options are summarized with the aim to help clinicians with diagnostic and therapeutic decision-making. The diagnosis of erythema multiforme, that has an acute, self-limiting course, is based on its typical clinical picture of targetoid erythematous lesions with predominant acral localization as well as histological findings...
January 19, 2018: Clinical Reviews in Allergy & Immunology
https://www.readbyqxmd.com/read/29352161/the-action-of-a-negative-allosteric-modulator-at-the-dopamine-d2-receptor-is-dependent-upon-sodium-ions
#14
Christopher J Draper-Joyce, Ravi Kumar Verma, Mayako Michino, Jeremy Shonberg, Anitha Kopinathan, Carmen Klein Herenbrink, Peter J Scammells, Ben Capuano, Ara M Abramyan, David M Thal, Jonathan A Javitch, Arthur Christopoulos, Lei Shi, J Robert Lane
Sodium ions (Na+) allosterically modulate the binding of orthosteric agonists and antagonists to many class A G protein-coupled receptors, including the dopamine D2 receptor (D2R). Experimental and computational evidences have revealed that this effect is mediated by the binding of Na+ to a conserved site located beneath the orthosteric binding site (OBS). SB269652 acts as a negative allosteric modulator (NAM) of the D2R that adopts an extended bitopic pose, in which the tetrahydroisoquinoline moiety interacts with the OBS and the indole-2-carboxamide moiety occupies a secondary binding pocket (SBP)...
January 19, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29352069/identification-of-ketene-reactive-intermediate-of-erlotinib-possibly-responsible-for-inactivation-of-p450-enzymes
#15
Huimin Zhao, Siyuan Li, Zixin Yang, Ying Peng, Xiaohui Chen, Jiang Zheng
Erlotinib (ELT), a tyrosine kinase inhibitor, is widely used for the treatment of non-small-cell lung cancer in clinic. Unfortunately, severe drug-induced liver injury and other adverse effects occurred during the treatment. Meanwhile, ELT has been reported to be a mechanism-based inactivator of CYPs 3A4 and 3A5. The objectives of this study were to identify ketene intermediate of ELT and investigate the association of the acetylenic bioactivation with the enzyme inactivation caused by ELT. A ketene intermediate was detected in human microsomal incubations of ELT, using 4-bromobenzylamine as a trapping agent...
January 19, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29351800/drug-resistance-genes-pvcrt-o-and-pvmdr-1-polymorphism-in-patients-from-malaria-endemic-south-western-coastal-region-of-india
#16
Shiny Joy, Benudhar Mukhi, Susanta K Ghosh, Rajeshwara N Achur, D Channe Gowda, Namita Surolia
BACKGROUND: Malaria is highly prevalent in many parts of India and is mostly caused by the parasite species Plasmodium vivax followed by Plasmodium falciparum. Chloroquine (CQ) is the first-line treatment for blood stage P. vivax parasites, but cases of drug resistance to CQ have been reported from India. One of the surveillance strategies which is used to monitor CQ drug resistance, is the analysis of single nucleotide polymorphisms (SNPs) of the associated gene markers. Susceptibility to CQ can also be determined by copy number assessment of multidrug resistant gene (mdr-1)...
January 19, 2018: Malaria Journal
https://www.readbyqxmd.com/read/29351470/increased-pro-renin-receptor-expression-in-subfornical-organ-neurons-in-hypertensive-humans
#17
Silvana G Cooper, Darshan P Trivedi, Rieko Yamamoto, Caleb J Worker, Cheng-Yuan Feng, Jacob T Sorensen, Wei Yang, Zhenggang Xiong, Yumei Feng
The central nervous system plays an important role in essential hypertension in humans and in animal models of hypertension through modulation of sympathetic activity, and sodium and body fluid homeostasis. Data from animal models of hypertension suggest that the renin-angiotensin system in the subfornical organ (SFO) of the brain is critical for hypertension development. We recently reported that the brain (pro)renin receptor (PRR) is a novel component of the brain renin-angiotensin system and could be a key initiator of the pathogenesis of hypertension...
December 22, 2017: American Journal of Physiology. Heart and Circulatory Physiology
https://www.readbyqxmd.com/read/29351433/%C3%AE-nitrostyrene-derivatives-attenuate-lps-mediated-acute-lung-injury-via-the-inhibition-of-neutrophil-platelet-interactions-and-net-release
#18
Yao-Wen Chang, Ching-Ping Tseng, Chih-Hsun Lee, Tsong-Long Hwang, Yu-Li Chen, Mei-Tzu Su, Kowit-Yu Chong, Ying-Wei Lan, Chin-Chung Wu, Kung-Ju Chen, Fen-Hua Lu, Hsiang-Ruei Liao, Chuen Hsueh, Pei-Wen Hsieh
Acute lung injury (ALI) and the acute respiratory distress syndrome (ARDS) are high-mortality and life-threatening diseases that are associated with neutrophil activation and accumulation within lung tissue. Emerging evidence indicates that neutrophil-platelet aggregates (NPAs) at sites of injury increases acute inflammation and contributes to the development of ALI. Even though numerous studies have increased our understanding of the pathophysiology of ALI, there is still a lack of innovative and useful treatments that reduce mortality, emphasizing that there is an urgent need for novel treatment strategies...
January 11, 2018: American Journal of Physiology. Lung Cellular and Molecular Physiology
https://www.readbyqxmd.com/read/29351056/remediation-of-radiation-induced-cognitive-dysfunction-through-oral-administration-of-the-neuroprotective-compound-nsi-189
#19
Barrett Allen, Munjal M Acharya, Celine Lu, Erich Giedzinski, Nicole Chmielewski, David Quach, Mike Hefferan, Karl K Johe, Charles L Limoli
Clinical management of primary and secondary central nervous system (CNS) malignancies frequently includes radiotherapy to forestall tumor growth and recurrence after surgical resection. While cranial radiotherapy remains beneficial, adult and pediatric brain tumor survivors suffer from a wide range of debilitating and progressive cognitive deficits. Although this has been recognized as a significant problem for decades, there remains no clinical recourse for the unintended neurocognitive sequelae associated with these types of cancer treatments...
January 19, 2018: Radiation Research
https://www.readbyqxmd.com/read/29350495/the-current-landscape-of-3d-in-vitro-tumor-models-what-cancer-hallmarks-are-accessible-for-drug-discovery
#20
REVIEW
Darren Rodenhizer, Teresa Dean, Elisa D'Arcangelo, Alison P McGuigan
Cancer prognosis remains a lottery dependent on cancer type, disease stage at diagnosis, and personal genetics. While investment in research is at an all-time high, new drugs are more likely to fail in clinical trials today than in the 1970s. In this review, a summary of current survival statistics in North America is provided, followed by an overview of the modern drug discovery process, classes of models used throughout different stages, and challenges associated with drug development efficiency are highlighted...
January 19, 2018: Advanced Healthcare Materials
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