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https://www.readbyqxmd.com/read/28537942/locomotor-and-discriminative-stimulus-effects-of-four-novel-hallucinogens-in-rodents
#1
Michael B Gatch, Sean B Dolan, Michael J Forster
There has been increasing use of novel synthetic hallucinogenic compounds, 2-(4-bromo-2,5-dimethoxyphenyl)-N-(2-methoxybenzyl)ethanamine hydrochloride (25B-NBOMe), 2-(4-chloro-2,5-dimethoxyphenyl)-N-(2-methoxybenzyl)ethanamine hydrochloride (25C-NBOMe), 2-(4-iodo-2,5-dimethoxyphenyl)-N-(2-methoxybenzyl)ethanamine hydrochloride (25I-NBOMe), and N,N-diallyl-5-methoxy tryptamine (5-MeO-DALT), which have been associated with severe toxicities. These four compounds were tested for discriminative stimulus effects similar to a prototypical hallucinogen (-)-2,5-dimethoxy-4-methylamphetamine (DOM) and the entactogen (±)-3,4-methylenedioxymethamphetamine (MDMA)...
May 19, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28534885/modeling-combination-hcv-prevention-among-hiv-infected-men-who-have-sex-with-men-and-people-who-inject-drugs
#2
Natasha K Martin, Britt Skaathun, Peter Vickerman, David Stuart
People who inject drugs (PWID) and HIV-infected men who have sex with men (MSM) are key risk groups for HCV transmission. Mathematical modeling studies can help elucidate what level and combination of prevention intervention scale-up is required to control or eliminate epidemics among these key populations. We discuss the evidence surrounding HCV prevention interventions and provide an overview of the mathematical modeling literature projecting the impact of scaled-up HCV prevention among PWID and HIV-infected MSM...
May 23, 2017: AIDS Reviews
https://www.readbyqxmd.com/read/28532300/engineered-polymeric-amphiphiles-self-assembling-into-nanostructures-and-acting-as-efficient-gene-and-drug-carriers
#3
Ruby Bansal, Pradeep Kumar
Nonviral gene delivery systems are finding widespread use due to their safety, rapid and economical production, and ease of modification. In this work, series of N-alkyl-substituted linear polyethylenimine (CP) polymers have been synthesized, characterized, and investigated about how degree of substitution (hydrophobic-hydrophilic balance) (i.e. N-alkylation) influenced the transfection efficiency. Mobility shift assay demonstrated efficient binding of plasmid DNA (pDNA). Transfection efficiency and cytotoxicity of CP polymers were assessed in vitro, which revealed that all the formulations exhibited higher transfection activity than linear polyethylenimine (lPEI) and commercial transfection reagents, Lipofectamine and Superfect, with negligible toxicity (MTT assay)...
January 1, 2017: Journal of Biomaterials Applications
https://www.readbyqxmd.com/read/28532282/synthesis-of-ph-responsive-n-acetyl-cysteine-modified-starch-derivatives-for-oral-delivery
#4
Kwanghyok Jong, Benzhi Ju, Shufen Zhang
In this study, a novel type of pH-responsive polymer PyHES-NAC ((2-hydroxy-3-(2-propynyloxy) propyl hydroxyethyl starch (PyHES)) - (N-Acetyl-cysteine (NAC)) was synthesized. First, PyHES was prepared via hydrophobic modification of hydroxyl groups in hydroxyethyl starch (HES) with propynylglycidyl ether (PGE), and then pH-responsive carboxylic acid group was connected to propynyl group via thiol-yne click reaction with NAC. Aqueous PyHES-NAC solutions exhibited a good transference between hydrophobic (or self-assembly) and hydrophilic static along with the change of pH value and protective properties of drugs under acidic conditions...
May 22, 2017: Journal of Biomaterials Science. Polymer Edition
https://www.readbyqxmd.com/read/28532049/co-delivery-of-cisplatin-and-doxorubicin-from-calcium-phosphate-beads-matrix-scaffolds-for-osteosarcoma-therapy
#5
Ulrike Hess, Shakiba Shahabi, Laura Treccani, Philipp Streckbein, Christian Heiss, Kurosch Rezwan
Bone substitute materials with a controlled drug release ability can fill cavities caused by the resection of bone tumours and thereby combat any leftover bone cancer cells. The combined release of different cytostatics seems to enhance their toxicity. In this study, calcium phosphate beads and matrix scaffolds are combined for a long-term co-delivery of cis-diamminedichloroplatinum (cisplatin, CDDP) and doxorubicin hydrochloride (DOX) as clinical relevant model drugs. Tricalcium phosphate/alginate beads as additional drug carrier are produced by droplet extrusion with ionotropic gelation and incorporated in scaffold matrix by freeze gelation without sintering...
August 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28532011/molecularly-imprinted-polymer-for-human-viral-pathogen-detection
#6
REVIEW
Aijaz Ahmad Malik, Chanin Nantasenamat, Theeraphon Piacham
Molecular imprinting has become an attractive synthetic approach for the fabrication of novel functional polymers with pre-designed molecular target selectivity. Such molecularly imprinted polymers (MIPs) have been applied in wide range of areas such as chemical and biological sensors, solid phase extraction and drug assays owing to their inherent robustness, reusability and reproducibility. Furthermore, MIPs can also be used as tools for studies concerning antibody/receptor binding site mimicry as well as being used as antibody substitutes for biomedical applications...
August 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28531991/multifunctional-polymer-drug-loading-system-with-ph-sensitive-fluorescent-and-targeting-property
#7
Xuening Fei, Shubei Li, Lingyun Cao, Baolian Zhang, Miaozhuo Yu
IA multifunctional drug loading system with pH-sensitive, fluorescent and targeting property was fabricated. Firstly, the amphipathic N-octyl-N'-(2-carboxyl-cyclohexamethenyl) chitosan (OCCC) was prepared by grafting hydrophobic octyl group and hydrophilic hexahydrophthalic anhydride onto chitosan, then it was modified with folic acid (FA) and thiazole orange (TO) using polyethylene glycol (PEG) as the link to fabricate a multifunctional drug loading system TO-PEG-OCCC-PEG-FA. Its chemical structure was determined by Fourier transform infrared spectroscopy (FT-IR), elemental analysis, differential scanning calorimetry (DSC) analysis, UV-vis and fluorescence spectrometer, and the results showed that the substitution degree of hydrophobic/hydrophilic group onto chitosan were 41...
August 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28531980/self-assembled-nanomicelles-of-damnacanthal-loaded-amphiphilic-modified-chitosan-preparation-characterization-and-cytotoxicity-study
#8
Pakin Sukamporn, Seung Joon Baek, Wandee Gritsanapan, Suwabun Chirachanchai, Thararat Nualsanit, Pleumchitt Rojanapanthu
Damnacanthal (Dam) is a phytochemical with many pharmacological properties including anticancer activity. However, its hydrophobicity, poor bioavailability and stability limit its application in many biological approaches. In this study, Dam nanomicelles as an emerging platform were developed to overcome limitations. The deoxycholic and poly(ethylene glycol) methyl ether grafted chitosan (DCA-CS-mPEG) was synthesized and characterized by FTIR and (1)H NMR and the degree of substitution (DS) was determined by elemental analysis (EA)...
August 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28531095/synthesis-of-1-2-3-triazolo-4-5-h-quinolone-derivatives-with-novel-anti-microbial-properties-against-metronidazole-resistant-helicobacter-pylori
#9
Mohammad Abu-Sini, Amal Mayyas, Nehaya Al-Karablieh, Rula Darwish, Yusuf Al-Hiari, Talal Aburjai, Shereen Arabiyat, Luay Abu-Qatouseh
Helicobacter pylori infection can lead to gastritis, peptic ulcer, and the development of mucosa associated lymphoid tissue (MALT) lymphoma. Treatment and eradication of H. pylori infection can prevent relapse and accelerate the healing of gastric and duodenal ulcers as well as regression of malignancy. Due to the increasing emergence of antibiotic resistance among clinical isolates of H. pylori, alternative approaches using newly discovered antimicrobial agents in combination with the standard antibiotic regimens for the treatment of H...
May 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28529359/the-journey-of-opioid-substitution-therapy-in-india-achievements-and-challenges
#10
Ravindra Rao
Opioids are one of the most problematic illegal substances globally. Opioid abuse is associated with complications in various spheres of the user's life, his/her family, and the society. Injecting drug use (IDU) is also linked to public health problems such as HIV infection and viral hepatitis. Medications form an important cornerstone in the treatment of opioid dependence. Treatment strategies such as "detoxification" alone or long-term treatment with opioid antagonist have limited acceptability and retention rates...
January 2017: Indian Journal of Psychiatry
https://www.readbyqxmd.com/read/28527822/synthesis-and-biological-evaluation-of-new-c-12-%C3%AE-%C3%AE-n-sulfamoyl-phenylamino-14-deoxy-andrographolide-derivatives-as-potent-anti-cancer-agents
#11
Sai Giridhar Sarma Kandanur, Srinivas Nanduri, Nageswara Rao Golakoti
Andrographolide, the major diterpenoidal constituent of Andrographis paniculata (Acanthaceae) and its derivatives have been reported to possess plethora of biological properties including potent anti-cancer activity. In this work, synthesis and in-vitro anti-cancer evaluation of new C-12-substituted aryl amino 14-deoxy-andrographolide derivatives (III a-f) are reported. The substitutions include various sulfonamide moieties -SO2-NH-R(1). The new derivatives (III a-e) exhibited improved cytotoxicity (GI50, TGI and LC50) compared to andrographolide (I) and the corresponding 3,14,19-O-triacetyl andrographolide (II) when evaluated against 60 NCI cell line panel...
April 13, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28526743/systematic-identification-of-functional-residues-of-artemisia-annua-amorpha-4-11-diene-synthase
#12
Xin Fang, Jian-Xu Li, Jin-Quan Huang, You-Li Xiao, Peng Zhang, Xiao-Ya Chen
Terpene synthases (TPSs) are responsible for the extremely diversified and complex structure of terpenoids. Amorpha-4,11-diene synthase (ADS) has a high (90%) fidelity in generating the sesquiterpene precursor for biosynthesis of artemisinin, an antimalarial drug, however, little is known about how active site residues of ADS involved in the carbocation rearrangement and cyclization reactions. Here, we identify seven residues that are key to most of the catalytic steps in ADS. By structural modeling and amino acid sequence alignments of ADS with two functionally relevant sesquiterpene synthases from Artemisia annua, we performed site-directed mutagenesis and found that a single substitution, T296V, impaired the ring closure activity almost completely, and tetra-substitutions (L374Y/L404V/L405I/G439S) led to an enzyme generating 80% monocyclic bisabolyl-type sesquiterpenes, whereas a double mutant (T399L/T447G) showed compromised activity in regioselective deprotonation to yield 34...
May 19, 2017: Biochemical Journal
https://www.readbyqxmd.com/read/28526350/designing-novel-bioconjugates-of-hydroxyethylcellulose-and-salicylates-for-potential-pharmaceutical-and-pharmacological-applications
#13
Khawar Abbas, Muhammad Amin, Muhammad Ajaz Hussain, Muhammad Sher, Syed Nasir Abbas Bukhari, Ibrahim Jantan, Kevin J Edgar
The present study deals with fabrication of macromolecular prodrugs (MPDs) of salicylic acid (SA) and aspirin (ASP) based on a hydrophilic cellulose ether, hydroxyethylcellulose (HEC). Degrees of substitution (DS) of SA and ASP per HEC repeating unit (HEC-RU) were achieved ranging from 0.60-2.18 and 0.53-1.50, respectively. The amphiphilic HEC-SA conjugate 2 assembled into nanowire-like structures, while HEC-ASP conjugate 6 formed nanoparticles (diameter 300-700nm) at a water/DMSO interface. After oral administration in rabbit models, conjugates 2 and 6 showed plasma half-life of 6...
May 16, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28524293/the-contribution-of-direct-patient-reported-adrs-to-drug-safety-signals-in-the-netherlands-from-2010-to-2015
#14
Florence van Hunsel, Susan de Waal, Linda Härmark
PURPOSE: The purpose of this study was to investigate the contribution of patient reports to signals sent by the Netherlands Pharmacovigilance Centre Lareb to the Dutch Medicines Evaluation Board and to determine if there are certain types of signals where patient report add a distinct contribution. METHOD: All signals from 2010 until 2015 were included. First, we investigated how many patient reports were present in the signals and the characteristics of these reports compared to the health care professional and marketing authorization holders' reports...
May 19, 2017: Pharmacoepidemiology and Drug Safety
https://www.readbyqxmd.com/read/28523110/photodynamic-activities-of-porphyrin-derivative-cyclodextrin-complexes-by-photoirradiation
#15
Atsushi Ikeda, Shuhei Satake, Tomoya Mae, Masafumi Ueda, Kouta Sugikawa, Hajime Shigeto, Hisakage Funabashi, Akio Kuroda
Water-soluble cyclodextrin (CyD) complexed with porphyrin derivatives with different substituents in the meso-positions showed different photodynamic activities toward cancer cells under illumination at wavelengths over 600 nm, the most suitable wavelengths for photodynamic therapy (PDT). In particular, aniline- and phenol-substituted derivatives had high photodynamic activity because of the efficient intracellular uptake of the complexes by tumor cells. These complexes showed greater photodynamic activity than photofrin, currently the main drug in clinical use as a photosensitizer...
May 11, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28523101/design-and-synthesis-of-potent-and-selective-pim-kinase-inhibitors-by-targeting-unique-structure-of-atp-binding-pocket
#16
Hirofumi Nakano, Tsukasa Hasegawa, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano
In the development of kinase inhibitors, one of the major concerns is selectivity. An effective strategy to achieve high selectivity is to utilize structural differences among kinases to inform inhibitor design. Here, we set out to improve the PIM (proviral integration site for Moloney murine leukemia virus) kinase-inhibitory selectivity of our previously reported 7-azaindole derivative 2, which has promising ADMET properties, by targeting a unique bulge in the ATP-binding pocket. 6-Substituted 7-azaindoles, especially the 6-chlorinated derivatives, proved to be potent and selective PIM kinase inhibitors and appear to be promising lead compounds for future drug discovery...
May 11, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28522372/effective-antimicrobial-activity-of-a-peptide-mutant-cbf-14-2-against-penicillin-resistant-bacteria-based-on-its-unnatural-amino-acids
#17
Wei Kang, Hanhan Liu, Lingman Ma, Mengxiao Wang, Shanshan Wei, Pengbo Sun, Meiling Jiang, Min Guo, Changlin Zhou, Jie Dou
Broad spectrum activities, a unique mode of actions and rare resistant variants make antimicrobial peptide (AMP) a potential alternative to antibiotics. However, AMPs still have limitations in clinical development due to their physiological stability, toxicity and manufacturing costs. Cbf-14, derived from cathelicidin-BF has been proven to be effective against drug-resistant bacteria. Herein, a series of Cbf-14 mutants were designed to overcome these limitations. Design strategies included substitutions of lysine (Lys) or leucine (Leu) with similar residues such as ornithine (Orn) and norleucine (Ile), which are unnatural amino acids, to generate AMPs with enhanced therapeutic potential...
May 15, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28521955/prevalence-of-relevant-ns5a-resistance-associated-substitutions-to-elbasvir-in-genotype-1a-hepatitis-c-virus-patients-in-spain
#18
Claudia Palladino, Beatriz Esteban-Cartelle, Irene Mate-Cano, Marta Sánchez-Carrillo, Salvador Resino, Verónica Briz
Resistance-associated substitutions (RASs) to the new HCV NS5A inhibitor elbasvir may limit its efficacy and lead to virological failure in HCV-GT1a-infected patients. There are no data outside clinical trials evaluating their prevalence and impact in grazoprevir/elbasvir in GT1a-infected patients in Spain. A multicentre cross-sectional study of 632 initial patients was conducted. In 13 of these patients, the sample could not be amplified or a consensus sequence by Sanger sequencing could not be performed. Ultimately, 617 HCV-G1a-infected individuals treated at 84 Spanish hospitals from the 17 autonomous communities plus the 2 autonomous cities of Spain were analysed...
May 15, 2017: Enfermedades Infecciosas y Microbiología Clínica
https://www.readbyqxmd.com/read/28520511/upregulation-of-acref-in-quinolone-resistance-development-in-escherichia-coli-when-acrab-tolc-function-is-impaired
#19
Chuan-Zhen Zhang, Man-Xia Chang, Lei Yang, Yan-Yan Liu, Pin-Xian Chen, Hong-Xia Jiang
We studied mechanisms of drug resistance development in Escherichia coli strains lacking efflux pump components. E. coli K12 deletion mutants were subjected to increasing concentrations of ciprofloxacin (CIP) to determine the frequency of target gene mutations. We generated a series of mutants that were selected based on their minimum inhibitory concentrations (MICs) to CIP, as well as their corresponding point mutations in target genes. The mutants displayed a number of target modifications and, in particular, gyrA mutations altering codons Ser83Leu, Asp87Gly, and Asp87His as well as a change in parC at 78 (substitution of Gly for Asp)...
May 18, 2017: Microbial Drug Resistance: MDR: Mechanisms, Epidemiology, and Disease
https://www.readbyqxmd.com/read/28520509/recent-advances-in-electrospun-nanofibers-for-wound-healing
#20
Shixuan Chen, Bing Liu, Mark A Carlson, Adrian F Gombart, Debra A Reilly, Jingwei Xie
Electrospun nanofibers represent a novel class of materials that show great potential in many biomedical applications including biosensing, regenerative medicine, tissue engineering, drug delivery and wound healing. In this work, we review recent advances in electrospun nanofibers for wound healing. This article begins with a brief introduction on the wound, and then discusses the unique features of electrospun nanofibers critical for wound healing. It further highlights recent studies that have used electrospun nanofibers for wound healing applications and devices, including sutures, multifunctional dressings, dermal substitutes, engineered epidermis and full-thickness skin regeneration...
May 18, 2017: Nanomedicine
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