962,295 results match your criteria Pharmaceutical Development and Technology [Journal]


[The Rezūm system in the treatment of male lower urinary tract symptoms (LUTSs) due to benign prostatic obstruction (BPO)].

Aktuelle Urol 2018 Dec 6;49(6):519-524. Epub 2018 Dec 6.

Spital Thurgau AG, Urologie, Frauenfeld.

The classical algorithm of the management of male lower urinary tract symptoms (LUTSs) due to benign prostatic hyperplasia (BPH) includes a surgical approach in case pharmacological therapy has failed. Emerging minimally-invasive treatments (MITs) offer potential for rapid symptomatic relief, reducing the morbidity of invasive BPH surgery. Convective interstitial radiofrequency water vapour thermal ablation of the prostate with the Rezūm system is a novel MIT for the treatment of bothersome moderate-to-severe lower urinary tract symptoms associated with BPH. Read More

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December 2018
8 Reads

High Circulating Alarin Levels Are Associated with Presence of Metabolic Syndrome.

Cell Physiol Biochem 2018 Dec 6;51(5):2041-2051. Epub 2018 Dec 6.

Department of Endocrinology, the Second Affiliated Hospital, Chongqing Medical University and Chongqing Clinical Research Center for Geriatrics, Chongqing,

Background/aims: Alarin has been reported to be related with increased food intake and body weight. The relationship of circulating Alarin with insulin resistance or metabolic syndrome (MetS), however, is unknown. This study aimed to investigate the physiological role of Alarin and its association with MetS in humans. Read More

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December 2018
1 Read

Simultaneous analysis of acetylcarnitine, proline, hydroxyproline, citrulline, and arginine as potential plasma biomarkers to evaluate NSAIDs-induced gastric injury by liquid chromatography-tandem mass spectrometry.

J Pharm Biomed Anal 2018 Nov 24;165:101-111. Epub 2018 Nov 24.

School of Pharmacy, Sungkyunkwan University, Suwon, Republic of Korea. Electronic address:

Although major adverse effects associated with nonsteroidal anti-inflammatory drugs (NSAIDs) are gastric injury, assessment of NSAIDs-induced gastrointestinal adverse effects is mostly dependent on endoscopy due to the lack of plasma biomarkers. Several amino acids associated with collagenase activity and gastric mucosal mass have been suggested as plasma biomarker candidates for gastric injury. Therefore, this study aimed to develop a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for the plasma biomarker candidates, i. Read More

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November 2018
2 Reads

Discovery and development of small molecule modulators targeting glutamine metabolism.

Eur J Med Chem 2018 Nov 28;163:215-242. Epub 2018 Nov 28.

Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China. Electronic address:

Cancer cells have been confirmed diverge significantly from normal cells on the metabolic properties. Energy production in cancer cells is abnormally dependent on the glycolysis pathway and other atypical metabolic characteristics such as increased fatty acid synthesis and increased rates of glutamine metabolism. Among these metabolic features of cancers, glutamine metabolism has been reported to be the main energy supply for the growth and viability of a potentially large subset of malignant tumors. Read More

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November 2018
5 Reads
3.447 Impact Factor

Neuroprotective effects of a novel carnosine-hydrazide derivative on hippocampal CA1 damage after transient cerebral ischemia.

Eur J Med Chem 2018 Nov 28;163:207-214. Epub 2018 Nov 28.

Department of Neurosurgery, Kurume University, School of Medicine, Fukuoka, Japan. Electronic address:

Ischemia-reperfusion injuries produce reactive oxygen species that promote the peroxide lipid oxidation process resulting in the production of an endogenic lipid peroxide, 4-hydroxy-trans-2-nonenal (4-HNE), a highly cytotoxic aldehyde that induces cell death. We synthesized a novel 4-HNE scavenger - a carnosine-hydrazide derivative, l-carnosine hydrazide (CNN) - and examined its neuroprotective effect in a model of transient ischemia. PC-12 cells were pre-incubated with various doses (0-50 mmol/L) of CNN for 30 min, followed by incubation with 4-HNE (250 μM). Read More

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November 2018
1 Read

Seasonal occurrence and fate of chiral pharmaceuticals in different sewage treatment systems in Hong Kong: Mass balance, enantiomeric profiling, and risk assessment.

Water Res 2018 Nov 9;149:607-616. Epub 2018 Nov 9.

State Key Laboratory of Marine Pollution (SKLMP), Research Centre for the Oceans and Human Health, Shenzhen Key Laboratory for the Sustainable Use of Marine Biodiversity, City University of Hong Kong, Hong Kong, China; Department of Chemistry, City University of Hong Kong, Hong Kong, China. Electronic address:

Concern about the presence of chiral pharmaceuticals in the environment from wastewater discharge is mounting. In this work, the occurrence and fate of atenolol, metoprolol, venlafaxine, and chloramphenicol, including 10 different stereoisomers, were investigated in sewage and sludge from diverse treatment processes in 4 sewage treatment plants (STPs) in Hong Kong via 4 sampling campaigns over a period of 2 years. The average amounts of individual pharmaceuticals entering the STPs ranged from 4. Read More

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November 2018
2 Reads

Effects of anterior tongue strengthening exercises on posterior tongue strength in healthy young adults.

Arch Oral Biol 2018 Nov 28;98:238-242. Epub 2018 Nov 28.

Kawasaki University of Medical Welfare, 288 Matsushima, Kurashiki, Okayama 701-0193, Japan. Electronic address:

Objective: The aim of the present study was to investigate whether anterior tongue muscle strengthening exercises can affect the strength of posterior tongue muscles.

Design: Eleven healthy subjects (20.6 ± 1. Read More

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November 2018
1 Read

Er Shen Wan extract alleviates polyuria and regulates AQP 2 and AVPR 2 in a rat model of spleen-kidney Yang deficiency-induced diarrhea.

Biomed Pharmacother 2018 Dec 3;110:302-311. Epub 2018 Dec 3.

College of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 610075, PR China; Sichuan Neo-Green Pharmaceutical Technology Development Co., Ltd, Chengdu 610081, PR China. Electronic address:

Ethnopharmacological Relevance: Er Shen Wan (ESW), has been empirically used for treating spleen-kidney Yang deficiency (SKYD) syndrome in Traditional Chinese medicine (TCM) for centuries and shows a variety of activities. The medicinal formula is a mixture of two component herbs, Psoraleae Fructus (PF, Bu-Gu-Zhi in Chinese) and Myristicae Semen (MS, Rou-Dou-Kou in Chinese). The current study was designed to evaluate ESWP antidiuretic treatment of polyuria and to explore potential mechanisms of renal water metabolism in the rat model of SKYD-induced diarrhea. Read More

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December 2018
1 Read

Food up-take and reproduction performance of Daphnia magna under the exposure of Bisphenols.

Ecotoxicol Environ Saf 2018 Dec 3;170:47-54. Epub 2018 Dec 3.

Key laboratory of Drug Quality Control and Pharmacovigilance (Ministry of Education) & School of Engineering, China Pharmaceutical University, Nanjing 211198, China. Electronic address:

Because the application of Bisphenol A (BPA) was restricted, many substitutes, such as Bisphenol F (BPF) and Bisphenol S (BPS), were developed as BPA substitutes. Therefore, environmental impacts of BPA and its substitutes on aquatic organisms should be concerned, especially their combined toxicity. In this study, the impacts of BPA, BPF, BPS and their mixture on the feeding behavior, reproduction and physiological function of daphnids were synthetically evaluated, involving the duration and mode of exposure. Read More

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December 2018
3 Reads

Investigation on the binding of aloe-emodin with tyrosinase by spectral analysis and molecular docking.

Spectrochim Acta A Mol Biomol Spectrosc 2018 Nov 19;211:79-85. Epub 2018 Nov 19.

College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou 450001, PR China. Electronic address:

In this paper, the inhibitory kinetics of aloe-emodin on the activity of tyrosinase and the inhibitory mechanism have been investigated by using spectroscopic and molecular docking techniques. The results showed that aloe-emodin inhibited tyrosinase activity in a competitive manner. The binding constants, number of binding sites and thermodynamic parameters obtained at different temperature suggested that aloe-emodin spontaneously binds to tyrosinase at one binding site, mainly via electrostatic forces. Read More

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November 2018
1 Read

Genus Psoralea A review of the traditional and modern uses, phytochemistry and pharmacology.

J Ethnopharmacol 2018 Dec 3. Epub 2018 Dec 3.

CSIR-National Botanical Research Institute, Plant Transgenic Laboratory, P.O. Box 436, Rana Pratap Marg,Lucknow-226 001, U.P., India. Electronic address:

Ethnopharmacological Relevance: The genus Psoralea (Fabaceae) harbours 105 accepted species that are extensively used by local peoples and medicinal practitioners of China, India, and other countries for treatment of tooth decay, psoriasis, leucoderma, leprosy, kidney problems, tuberculosis, indigestion, constipation and impotence. Presently, pharmacological research reports are available on only few species namely Bituminaria bituminosa (Syn: P. bituminosa), P. Read More

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December 2018
8 Reads

Beneficial Effect of Curcumin Nanoparticles-Hydrogel on Excisional Skin Wound Healing in Type-I Diabetic Rat: Histological and Immunohistochemical Studies.

Ann Anat 2018 Dec 3. Epub 2018 Dec 3.

Department of Biochemistry, Faculty of Medicine, Cairo University, Cairo, Egypt.

Management of diabetic wounds remains a major challenge in the medical field, mostly due to incompetent outcomes of treatments. Curcumin has been documented as anti-inflammatory, antioxidant, antimicrobial and antineoplastic agent in addition to wound healing activities. However, its poor aqueous solubility and impaired skin permeation handicap its topical pharmaceutical usage. Read More

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December 2018
7 Reads

Characterization of A dextran-budesonide prodrug for inhalation therapy.

Eur J Pharm Sci 2018 Dec 3. Epub 2018 Dec 3.

Department of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville, FL 32610, United States of America. Electronic address:

Reducing the dosing frequency of corticosteroids may increase compliance and increase pulmonary targeting. The objective of this study was to evaluate whether a high molecular weight dextran-budesonide conjugate might be suitable for pulmonary slow release of the otherwise fast absorbed budesonide. An array of dextran-spacer-budesonide conjugates was prepared that differed in the molecular weight of dextran (20 kDa or 40 kDa) and the length of the dicarboxylic spacer (succinic, glutaric, and adipic anhydride). Read More

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December 2018
1 Read

Identifying critical process steps to protein stability during spray drying using a vibrating mesh or a two-fluid nozzle.

Eur J Pharm Sci 2018 Dec 3. Epub 2018 Dec 3.

Department of Pharmaceutical Technology and Biopharmacy, University of Groningen, Antonius Deusinglaan 1, 9713 AV Groningen, the Netherlands. Electronic address:

The aim of this study was to identify critical steps to protein stability during spray drying using two different nozzle types: a vibrating mesh nozzle and a standard two-fluid nozzle in a Büchi B-90 spray dryer. l-Lactic dehydrogenase was used as a model protein as it is a heat and shear stress sensitive protein. Trehalose was used as excipient because of its excellent stabilizing capacities. Read More

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December 2018

Radiochemical synthesis and preclinical evaluation of Ga-labeled NODAGA-hydroxypropyl-beta-cyclodextrin (Ga-NODAGA-HPBCD).

Eur J Pharm Sci 2018 Dec 3. Epub 2018 Dec 3.

Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei St. 98, H-4032 Debrecen, Hungary. Electronic address:

A new renaissance started in the research and application of cyclodextrins a few years ago. 2-Hydroxypropyl-beta-cyclodextrin (HPBCD) is used in the formulation of drugs and recently orphan designation was granted for the treatment of Niemann-Pick disease, type C. HPBCD is considered to be safe, but the exact mechanism of action and side effects are not completely explained. Read More

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December 2018
1 Read

Pharmaceutical cocrystals: from serendipity to design to application.

Drug Discov Today 2018 Dec 3. Epub 2018 Dec 3.

Synthesis and Solid State Pharmaceutical Centre (SSPC), Bernal Institute, University of Limerick, Limerick, Ireland. Electronic address:

The field of pharmaceutical cocrystals has reached a tipping point, particularly because cocrystals can improve the physicochemical properties of drugs without compromising their therapeutic benefit. Accounts of cocrystal investigations in the literature started in earnest in 2003 and patent applications soon followed. The frequency of both has steadily accelerated, demonstrating an enhanced understanding of the design, characterisation, and manufacture of cocrystals and heightened interest from industry. Read More

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December 2018
3 Reads

Preparation and optimization of poly (lactic acid) nanoparticles loaded with fisetin to improve anti-cancer therapy.

Int J Biol Macromol 2018 Dec 3. Epub 2018 Dec 3.

Department of Pharmaceutics, School of Pharmacy, Jiangsu University, Zhenjiang 212013, PR China. Electronic address:

Fisetin is a natural flavonoid with promising antitumor activity, whereas its clinical application is limited by its hydrophobic property. In this study, we aimed to load fisetin into poly(lactic acid) (PLA) nanoparticles to increase fisetin's solubility and therapeutic efficacy. Based on spontaneous emulsification solvent diffusion (SESD) method, the formulation of PLA nanoparticles was optimized by two successive experimental designs. Read More

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December 2018
2 Reads

Polyethylene glycol-decorated doxorubicin/carboxymethyl chitosan/gold nanocomplex for reducing drug efflux in cancer cells and extending circulation in blood stream.

Int J Biol Macromol 2018 Dec 3. Epub 2018 Dec 3.

College of Pharmacy, Gachon University, Incheon 21936, Republic of Korea. Electronic address:

Polyethylene glycol (PEG)-decorated doxorubicin (Dox)/carboxymethyl chitosan (CMC)/gold nanoparticles (AuNPs) have been developed for cancer therapy. CMC was used as a reducing and stabilizing agent for the fabrication of AuNPs and Dox was loaded onto AuNPs as a chemotherapeutic agent. Dox-loaded CMC-stabilized AuNPs (Dox/CMC-AuNPs) with a mean diameter of 104. Read More

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December 2018
4 Reads

The polyphenolic-polysaccharide complex of Agrimonia eupatoria L. as an indirect thrombin inhibitor - isolation and chemical characterization.

Int J Biol Macromol 2018 Dec 3. Epub 2018 Dec 3.

Department of Organic and Pharmaceutical Technology, Faculty of Chemistry, Wrocław University of Science and Technology, Wybrzeże Wyspiańskiego 29, 50-370 Wrocław, Poland; Regional Specialist Hospital in Wrocław, Research and Development Centre, Kamieńskiego 73a, 51-124 Wrocław, Poland.

The polyphenolic-polysaccharide complex was isolated from the dried aerial parts of the medicinal plant Agrimonia eupatoria L. using a multi-step process involving the degreasing of the plant material by extraction with organic solvents, followed by extraction with hot alkali, neutralization, further separation with organic solvents and dialysis. The complex was homogeneous with a molecular weight of about 55 × 10 g/mol and consisted mainly of carbohydrates and polyphenols matrix, composed of lignin-related units, with the dominance of dimethoxyphenyl structures. Read More

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December 2018
1 Read

Ammonium persulphate induced synthesis of polymethyl methacrylate grafted sodium alginate composite films with high strength for food packaging.

Int J Biol Macromol 2018 Dec 3. Epub 2018 Dec 3.

State Key Laboratory of Bio-Fibers and Eco-Textiles, Qingdao University, Qingdao 266071, PR China; College of Chemistry and Chemical Engineering, Qingdao University, Qingdao 266071, PR China. Electronic address:

The graft copolymerization of methyl methacrylate (MMA) onto alginate was carried out in aqueous media by initiators of ammonium persulphate under a nitrogen gas atmosphere. Then, the grafting of PMMA chains onto the alginate backbone was confirmed through the study of Fourier transform infrared, X-ray diffraction, scanning electron microscopy and H nuclear magnetic resonance spectroscopy. At last, a thin and transparent polymethyl methacrylate grafted alginate film with high strength was obtained by the casting method. Read More

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December 2018
2 Reads

Combined synergetic potential of metformin loaded pectin-chitosan biohybrids nanoparticle for NIDDM.

Int J Biol Macromol 2018 Dec 3. Epub 2018 Dec 3.

Department of Pharmaceutics, GITAM University, Rushikonda, Visakapatnam 530045, Andhra Pradesh, India.

Rationale: Combined therapy is a promising approach over its preference to minimize the dose, adverse effects and enhanced therapeutic efficiency in a various diseases including diabetes.

Aim: The present research work is to explore combined synergistic anti-diabetic potential of chitosan and pectin with Metformin (CPM) nano-formulation, with special emphasis on effect of Metformin when integrated with bio polymers.

Methods: The biohybrid nanoparticles (CPMNP) were formulated by ionic gelation process. Read More

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December 2018
1 Read

Pilot-scale isolation and characterization of extracellular polymeric substances (EPS) from cell-free medium of Spirulina sp. LEB-18 cultures under outdoor conditions.

Int J Biol Macromol 2018 Dec 3. Epub 2018 Dec 3.

College of Pharmacy, Federal University of Bahia, Salvador, Brazil.

This objective of this work was to monitor the EPS production during the growth of Spirulina sp. LEB-18, evaluate the productivity and to characterize the exopolymers obtained on pilot-scale under outdoor conditions. The production of crude EPS occurred in all phases of biomass growth and was approximately ten folds higher than that biomass concentration of Spirulina sp. Read More

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December 2018

Analysis of interaction between sulfated polysaccharides and HIV oligopeptides by surface plasmon resonance.

Int J Biol Macromol 2018 Dec 3. Epub 2018 Dec 3.

Department of Bio and Environmental Chemistry, Kitami Institute of Technology, 165 Koen-cho, Kitami, Hokkaido 090-8507, Japan. Electronic address:

This study aims to quantitatively investigate the interaction between sulfated polysaccharides with potent anti-HIV activity, dextran and curdlan sulfates with negatively charged sulfate groups, and poly-l-lysine as a model protein and oligopeptides from a HIV surface glycoprotein gp120 with positively charged amino acids using surface plasmon resonance (SPR) and dynamic light scattering (DLS) to elucidate the anti-HIV mechanism of sulfated polysaccharides. The apparent association- (k) and dissociation rate (k) constants of dextran and curdlan sulfates against poly-l-lysine were k = 6.92 × 10-2. Read More

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December 2018

The novel cationic cell-penetrating peptide PEP-NJSM is highly active against Staphylococcus epidermidis biofilm.

Int J Biol Macromol 2018 Dec 3. Epub 2018 Dec 3.

Laboratory of Molecular and Cellular Screening Processes, Centre of Biotechnology of Sfax, University of Sfax, Road Sidi Mansour km 6, PO BOX 1177, 3018 Sfax, Tunisia.

A cationic cell-penetrating peptide PEP-NJSM was identified in human virus proteomes by a screening of charge clusters in protein sequences generating cell penetrating peptides (CPP). PEP-NJSM was selectively active against Gram positive Staphylococcus epidermidis as antibacterial agent with MIC value of 128 μM compared to the Gram-negative Pseudomonas aeruginosa strain with MIC value exceeded 512 μM. The selected peptide exhibited an important anti-biofilm activity even at sub-MIC levels. Read More

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December 2018
1 Read

Targeting indoleamine-2,3-dioxygenase in cancer: Scientific rationale and clinical evidence.

Pharmacol Ther 2018 Dec 3. Epub 2018 Dec 3.

Unit of Internal Medicine, Department of Medicine, University of Perugia, Perugia, Italy. Electronic address:

Immunotherapy through immune checkpoint blockers (ICBs) is quickly transforming cancer treatment by improving patients' outcomes. However, innate and acquired resistance to ICBs remain a major challenge in clinical settings. Indoleamine 2,3-dioxygenases (IDOs) are enzymes involved in tryptophan catabolism with a central immunosuppressive function within the tumor microenvironment. Read More

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December 2018
2 Reads

Anticancer activity modulation of an innovative solid formulation of extra virgin olive oil by cultured zeolite scaffolds.

Food Chem Toxicol 2018 Dec 3. Epub 2018 Dec 3.

Research Institute on Membrane Technology, Unit of Zeolite Membranes, ITM-CNR, University of Calabria, Cubo 17/c, 87036, Rende, Italy.

This paper deals with the design and manufacture of pure and hybrid synthetic (Mixed Matrix Membranes, MMMs) zeolite scaffolds (containing various amount of zeolite crystals dispersed in a polymeric matrix) to obtain new biomaterials. These scaffolds can potentially be used in the field of translational medicine to obtain innovative results to address tumorigenesis mechanisms with the promotion of an effort to deal with technical methods and information. Since olive oil has beneficial effects in healthy human cells and slows down and/or inhibits cell growth, the aim of this work was to monitor the protective and beneficial antitumor effects of olive oil in a new solid formulation (Spread Bio-Oil) on cancer cell cultured on zeolite scaffolds. Read More

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December 2018

5-Azido-8-ethynyl-NAADP: A bifunctional, clickable photoaffinity probe for the identification of NAADP receptors.

Biochim Biophys Acta Mol Cell Res 2018 Dec 3. Epub 2018 Dec 3.

Department of Pharmacology, University of Minnesota Medical School, 312 Church St., Minneapolis, MN 55455-0217, United States of America. Electronic address:

Nicotinic acid adenine dinucleotide phosphate is an evolutionarily conserved second messenger, which mobilizes Ca from acidic stores. The molecular identity of the NAADP receptor has yet to be defined. In pursuit of isolating and identifying NAADP-binding proteins, we synthesized and characterized a bifunctional probe that incorporates both a photoactivatable crosslinking azido moiety at the 5-position of the nicotinic ring and a 'clickable' ethynyl moiety to the 8-adenosyl position in NAADP. Read More

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December 2018

Electro-acupuncture attenuates the mice premature ovarian failure via mediating PI3K/AKT/mTOR pathway.

Life Sci 2018 Dec 3. Epub 2018 Dec 3.

College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China; Key Laboratory of Acupuncture and Medicine Research of Ministry of Education, Nanjing University of Chinese Medicine, Nanjing 210023, China. Electronic address:

Aims: Electro-acupuncture (EA) is frequently recommended as a complementary therapy for premature ovarian failure (POF) in the clinical. However, little information exists about its potential treatment mechanisms. The study was designed to observe the effect of EA to ovarian function and fertility in POF mice model, and investigated its potential mechanisms on PI3K/AKT/mTOR signaling pathway. Read More

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December 2018

Antiasthmatic potential of Zizyphus jujuba Mill and Jujuboside B. - Possible role in the treatment of asthma.

Respir Physiol Neurobiol 2018 Dec 3. Epub 2018 Dec 3.

R.C. Patel Institute of Pharmaceutical Education & Research, Shirpur, Dhule, 425405, India.

Zizyphus jujuba Mill, a famous oriental traditional medicine, has been reported to exhibit diverse activities in biological systems including the respiratory system. However, a little information is available on its antiasthmatic activity. Jujuboside B (JB) is a natural saponin and one of the active constituent of fruits of Zizyphus jujuba. Read More

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December 2018

Renoprotective meroterpenoids from the fungus Ganoderma cochlear.

Fitoterapia 2018 Dec 3. Epub 2018 Dec 3.

Guangdong Key Laboratory for Genome Stability & Disease Prevention, School of Pharmaceutical Sciences, School of Medicine, Shenzhen University Health Science Center, Shenzhen 518060, People's Republic of China. Electronic address:

Nine multifarious new meroterpenoids, cochlearols E-M (1-9), along with seven known meroterpenoids 10-16, were isolated from the fruiting bodies of Ganoderma cochlear. Racemic 1, 6-8, 10 and 13 were separated by chiral HPLC. The structures were elucidated based on detailed spectroscopic analyses (HRESIMS, 1D/2D-NMR) and calculated electronic circular dichroism (ECD). Read More

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December 2018
1 Read

Nucleoside and N-acetyldopamine derivatives from the insect Aspongopus chinensis.

Fitoterapia 2018 Dec 3. Epub 2018 Dec 3.

Guangdong Key Laboratory for Genome Stability & Disease Prevention, School of Pharmaceutical Sciences, Shenzhen University Health Science Center, Shenzhen 518060, PR China. Electronic address:

Two new nucleoside derivatives, named asponguanosines A and B (1 and 2), three new N-acetyldopamine analogues, aspongamides C-E (3-5), one new sesquiterpene, aspongnoid D (6), and three known compounds were isolated from the medicinal insect Aspongopus chinensis. Their structures including absolute configurations were assigned by using spectroscopic methods and ECD and C NMR calculations. Biological activities of compounds 3-7 towards human cancer cells, COX-2, ROCK1, and JAK3 were evaluated. Read More

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December 2018
2 Reads

5- lipoxygenase (ALOX5): genetic susceptibility to type 2 diabetes and vitamin D effects on monocytes.

J Steroid Biochem Mol Biol 2018 Dec 3. Epub 2018 Dec 3.

Department of Internal Medicine I, Division of Endocrinology, Diabetes and Metabolism, Goethe University Hospital, Frankfurt am Main, Germany.

The arachidonate 5-lipoxygenase (ALOX5) pathway has been implicated in chronic inflammatory disease which may be influenced by vitamin D due to vitamin D response elements (VDRE). We investigated an ALOX5 polymorphism (rs4987105) in patients with type 2 diabetes (T2D) and the in vitro effects of calcitriol (1,25(OH)D) on ALOX5 metabolism in monocytes of T2D patients and healthy controls (HC). 533 T2D and 473 HC were genotyped for the rs4987105 polymorphism. Read More

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December 2018

Mechanistic role of the CREB-regulated transcription coactivator 1 in cardiac hypertrophy.

J Mol Cell Cardiol 2018 Dec 3. Epub 2018 Dec 3.

Department of Clinical Pharmacology and Toxicology, Cardiovascular Research Center, University Medical Center Hamburg-Eppendorf, Martinistr. 52, 20246 Hamburg, Germany; DZHK (German Center for Cardiovascular Research), Partner Site Hamburg, Kiel, Lübeck, Germany; Institute of Pharmacy, University of Hamburg, Bundesstr. 45, 20146 Hamburg, Germany. Electronic address:

The sympathetic nervous system is the main stimulator of cardiac function. While acute activation of the β-adrenoceptors exerts positive inotropic and lusitropic effects by increasing cAMP and Ca, chronically enhanced sympathetic tone with changed β-adrenergic signaling leads to alterations of gene expression and remodeling. The CREB-regulated transcription coactivator 1 (CRTC1) is activated by cAMP and Ca. Read More

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December 2018
2 Reads

Macro-Nanomedicine: Targeting the big Picture.

Authors:
Twan Lammers

J Control Release 2018 Dec 3. Epub 2018 Dec 3.

Department of Nanomedicine and Theranostics, Institute for Experimental Molecular Imaging, RWTH Aachen University Clinic, Aachen, Germany; Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences, Utrecht University, the Netherlands; Department of Targeted Therapeutics, Biomaterial Science and Technology, University of Twente, Enschede, the Netherlands. Electronic address:

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December 2018
1 Read

Activation of mitochondrial aldehyde dehydrogenase (ALDH2) by ALDA-1 reduces both the acquisition and maintenance of ethanol intake in rats: A dual mechanism?

Neuropharmacology 2018 Dec 3. Epub 2018 Dec 3.

Program of Molecular and Clinical Pharmacology, ICBM, Faculty of Medicine, University of Chile, Santiago, Chile.

A number of pre-clinical studies have shown that brain-generated acetaldehyde, the first metabolite of ethanol, exerts reinforcing effects that promote the acquisition of ethanol intake, while chronic intake maintenance appears to be mediated by alcohol-induced brain neuroinflammation/oxidative stress. Recently, it was described that N-(1,3-benzodioxol-5-ylmethyl)-2,6-dichlorobenzamide (ALDA-1) activates aldehyde dehydrogenase-2 (ALDH2), enzyme that catalyzes the oxidation of ethanol-derived acetaldehyde to acetate. The aim of this study was to determine the effects of ALDA-1 on both the acquisition and the maintenance of alcohol intake in alcohol-preferring UChB rats. Read More

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December 2018

Design, synthesis and anti-tumor evaluation of novel steroidal glycoconjugate with furoxan derivatives.

Steroids 2018 Dec 3. Epub 2018 Dec 3.

Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai, 201203, China. Electronic address:

In this study, eighteen novel steroidal-furoxan derivatives with 3-glycosyl or 3-methoxy moiety (12a-c, 13a-c, 17a-c, 26a-c, 27a-c and 28a-c) were synthesized and their anti-proliferative activity was evaluated against eight drug-sensitive and three drug-resistant cancer cell lines HeLa, A2780, LNCaP, PC-3, MDA-MB-231, MCF-7, SW480, A549, MCF-7/ADR, A2780/CDDP and A2780/T. Most of them displayed significant anti-cancer potency in vitro with IC values at the nanomole level. Among them, 3-methoxy steroidal-furoxan hybrids expressed much better activity than that of 3-glycosyl substitute ones, while estrane and 5α-H-androstane scaffold were slightly more favorable to the improvement of anti-proliferative activity. Read More

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December 2018
3 Reads

Small Heterodimer Partner and Fibroblast Growth Factor 19 Inhibit Expression of NPC1L1 in Mouse Intestine and Cholesterol Absorption.

Gastroenterology 2018 Dec 3. Epub 2018 Dec 3.

Department of Molecular and Integrative Physiology, University of Illinois at Urbana-Champaign, Urbana, IL 61801. Electronic address:

Background & Aims: The nuclear receptor subfamily 0 group B member 2 (NR0B2, also called SHP) is expressed at high levels in liver and intestine. Postprandial fibroblast growth factor 19 (human FGF19, mouse FGF15) signaling increases the transcriptional activity of SHP. We studied the functions of SHP and FGF19 in intestines of mice, including their regulation of expression of the cholesterol transporter NPC1-like intracellular cholesterol transporter 1 (NPC1L1) and cholesterol absorption. Read More

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December 2018
1 Read

A value proposition for trough level-based anti-TNFα drug dosing.

Clin Chim Acta 2018 Dec 3. Epub 2018 Dec 3.

Expert Center Clinical Chemistry Eindhoven, Eindhoven, the Netherlands; Clinical Laboratory, Máxima Medical Center, Veldhoven, the Netherlands.

Treatment of inflammatory bowel diseases and rheumatic disorders with anti-tumor necrosis factor alpha (TNFα) drugs is expensive, while a significant proportion of patients does not show adequate clinical response. Therapeutic drug monitoring (TDM) enables patient-specific anti-TNFα therapy. The role of laboratory tests in clinical care has recently been described in a value proposition framework. Read More

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December 2018
3 Reads

Cabazitaxel and Thymoquinone co-loaded Lipospheres as a Synergistic Combination for Breast Cancer.

Chem Phys Lipids 2018 Dec 3. Epub 2018 Dec 3.

Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research (NIPER), Hyderabad, 500037, India. Electronic address:

Cabazitaxel as microtubule inhibitor and thymoquinone as HDAC inhibitor affects the important genes like p53, STAT3, Bax, BCL-2, p21 and down regulation of NF-κB are reported for potential activity against breast tumors. However, poor aqueous solubility and permeability hinders the delivery of these drugs to target site. To address the delivery challenges cabazitaxel and thymoquinone co-loaded lipospheres were developed. Read More

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December 2018

Pharmacological interventions for acute hepatitis C infection.

Cochrane Database Syst Rev 2018 Dec 3;12:CD011644. Epub 2018 Dec 3.

Sheila Sherlock Liver Centre, Royal Free Hospital and the UCL Institute of Liver and Digestive Health, London, UK.

Background: Hepatitis C virus (HCV) is a single-stranded RNA (ribonucleic acid) virus that has the potential to cause inflammation of the liver. The traditional definition of acute HCV infection is the first six months following infection with the virus. Another commonly used definition of acute HCV infection is the absence of HCV antibody and subsequent seroconversion (presence of HCV antibody in a person who was previously negative for HCV antibody). Read More

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December 2018
1 Read

A simple DNAzyme-based fluorescent assay for Klebsiella pneumoniae.

Chembiochem 2018 Dec 6. Epub 2018 Dec 6.

University of California Irvine, Pharmaceutical Sciences, Sue and Bill Gross Stem Cell Research Center, Edwards Lifesciences Center for Advanced Cardiovascular Technology, Biomedical Engineering, 92697, Irvine, UNITED STATES.

Pathogenic bacteria pose a serious public health threat. Rapid and cost effective detection of such bacteria remains a major challenge. Here, we present a DNAzyme-based fluorescent paper sensor for Klebsiella pneumoniae. Read More

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December 2018
2 Reads

Rapid and substantial increases in anticoagulant use and expenditure in Australia following the introduction of new types of oral anticoagulants.

PLoS One 2018 6;13(12):e0208824. Epub 2018 Dec 6.

National Centre for Epidemiology and Population Health, Australian National University, Canberra, Australia.

Objectives: To quantify changes in anticoagulant use in Australia since the introduction of Non-vitamin K antagonist anticoagulants (NOACs) and to estimate government expenditure.

Design: Interrupted-time-series analysis quantifying anticoagulant dispensing, before and after first Pharmaceutical Benefits Scheme (PBS) NOAC listing in August 2009 for venous thromboembolism prevention; and expanded listing for stroke prevention in non-valvular atrial fibrillation (AF) in August 2013, up to June 2016. Estimated government expenditure on PBS-listed anticoagulants. Read More

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December 2018

Anthocyanins from Cornus kousa ethanolic extract attenuate obesity in association with anti-angiogenic activities in 3T3-L1 cells by down-regulating adipogeneses and lipogenesis.

PLoS One 2018 6;13(12):e0208556. Epub 2018 Dec 6.

Department of Biotechnology, Chonnam National University, Dun-Duk Dong, Yeosu, Chonnam, Korea.

Cornus kousa the Korean dogwood has been traditionally used in East Asia as therapeutic traditional medicine however biological activities of Cornus kousa have not been investigated previously. The aim of the present study was to evaluate anti-obesity activities coupled with anti-angiogenic activities of anthocyanins rich fraction of ethanolic leaf extract of Cornus kousa (ELECk) in HUVECs and 3T3- L1 cells. Dried plants leaves were extracted with 70% ethanol and anthocyanin fraction (AnT Fr) was obtained by eluting the ethanolic extract through non-polar macroporous resin and further purification by HPLC. Read More

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December 2018
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Extended cleavage specificities of mast cell proteases 1 and 2 from golden hamster: Classical chymase and an elastolytic protease comparable to rat and mouse MCP-5.

PLoS One 2018 6;13(12):e0207826. Epub 2018 Dec 6.

Department of Cell and Molecular Biology, Uppsala University, The Biomedical Center, Uppsala, Sweden.

Serine proteases constitute the major protein content of mast cell secretory granules. Here we present the extended cleavage specificity of two such proteases from the golden hamster, Mesocricetus auratus. Analysis by phage display technique showed that one of them (HAM1) is a classical chymase with a specificity similar to the human mast cell chymase. Read More

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December 2018
2 Reads

Effect estimate comparison between the prescription sequence symmetry analysis (PSSA) and parallel group study designs: A systematic review.

PLoS One 2018 6;13(12):e0208389. Epub 2018 Dec 6.

Groningen Research Institute of Pharmacy, unit PharmacoTherapy, -Epidemiology & -Economics, University of Groningen, Groningen, The Netherlands.

Prescription sequence symmetry analysis (PSSA), a case-only design introduced in 1996, has been increasingly used to identify unintentional drug effects, and has potential applications as a hypothesis-testing and a hypothesis-generating method, due to its easy application and effective control of time-invariant confounders. The aim of this study is to systematically compare effect estimates from the PSSA to effect estimates from conventional observational parallel group study designs, to assess the validity and constraints of the PSSA study design. We reviewed the MEDLINE, EMBASE, and Web of Science databases until February 2016 to identify studies that compared PSSA to a parallel group design. Read More

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December 2018

A pragmatic cluster randomised controlled trial of a tailored intervention to improve the initial management of suspected encephalitis.

PLoS One 2018 6;13(12):e0202257. Epub 2018 Dec 6.

Department of Clinical Infection, Microbiology and Immunology, Institute of Infection and Global Health, University of Liverpool, Liverpool, United Kingdom.

Objective: To determine whether a tailored multifaceted implementation strategy improves the initial management of patients with suspected encephalitis.

Design: Pragmatic two arm cluster randomised controlled trial.

Setting: Hospitals within the United Kingdom. Read More

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December 2018
6 Reads

Doping in sport - attitude and professional experience among physicians in Poland.

Folia Med Cracov 2018 ;58(3):35-47

Department of Food Chemistry and Nutrition, Faculty of Pharmacy Jagiellonian University Medical College, Kraków; Henryk Niewodniczański Institute of Nuclear Physics, Polish Academy of Science, Kraków, Poland.

Introduction: The history of using performance-enhancing substances (PES) is long and it goes back to ancient times. At present, PES are employed at all levels of sport competition, starting from Olympic level contestants to individuals recreationally involved in various sports disciplines.

Purpose: e objective of the study was examining the views on doping in sports in a group of physicians, together with evaluating the frequency of their contacts with this phenomenon, in their professional activities. Read More

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January 2018
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Laparoscopic sleeve gastrectomy and gastroesophageal reflux.

Rom J Intern Med 2018 Dec;56(4):227-232

"Carol Davila" University of Medicine and Pharmacy, Bucharest, Romania.

The prevalence of obesity is rising, becoming a medical problem worldwide. Also GERD incidence is higher in obese patients compared with normal weight, with an increased risk of 2.5 of developing symptoms and erosive esophagitis. Read More

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December 2018

Pancreas divisum: a reemerging risk factor for pancreatic diseases.

Authors:
Serghei Covantev

Rom J Intern Med 2018 Dec;56(4):233-242

Laboratory of Allergology and Clinical Immunology, "Nicolae Testemitanu" State University of Medicine and Pharmacy, Chisinau, Republic of Moldova.

Pancreas divisum (PD) is the most common developmental anatomic variant of pancreatic duct. The attention towards the PD has grown significantly since there are reports that this condition may cause acute relapsing pancreatitis, chronic pancreatitis and chronic abdominal pain syndrome. Furthermore, over the years, there have been multiple reports of PD associated with different types of tumors. Read More

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December 2018
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