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Journal of Pharmacy and Pharmacology

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https://www.readbyqxmd.com/read/27905105/endothelin-1-et-1-stimulates-carboxy-terminal-smad2-phosphorylation-in-vascular-endothelial-cells-by-a-mechanism-dependent-on-et-receptors-and-de-novo-protein-synthesis
#1
Narges Sharifat, Ghorban Mohammad Zadeh, Mohammad-Ali Ghaffari, Parisa Dayati, Danielle Kamato, Peter J Little, Hossein Babaahmadi-Rezaei
OBJECTIVE: G protein-coupled receptor (GPCR) agonists through their receptors can transactivate protein tyrosine kinase receptors such as epidermal growth factor receptor and serine/threonine kinase receptors most notably transforming growth factor (TGF)-β receptor (TβRI). This signalling mechanism represents a major expansion in the cellular outcomes attributable to GPCR signalling. This study addressed the role and mechanisms involved in GPCR agonist, endothelin-1 (ET-1)-mediated transactivation of the TβRI in bovine aortic endothelial cells (BAECs)...
December 1, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27905101/a-review-on-antiviral-activity-of-the-himalayan-medicinal-plants-traditionally-used-to-treat-bronchitis-and-related-symptoms
#2
REVIEW
Rahila Amber, Muhammad Adnan, Akash Tariq, Sakina Mussarat
OBJECTIVES: Bronchitis is a common respiratory tract infection of humans mainly caused by influenza virus, rhinovirus, adenovirus, coronavirus and respiratory syncytial virus. The aim of this review was to gather fragmented literature on ethnomedicinal plants used against bronchitis in the Himalayan region and their in-vitro validation against bronchitis causing viral pathogens. KEY FINDINGS: Present review contains ethnomedicines of total 55 plants from different countries of the Himalayas...
December 1, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27891611/pharmacokinetics-cannot-explain-the-increased-effective-dose-requirement-for-morphine-and-midazolam-in-rats-during-their-extended-administration-alone-or-in-combination
#3
Stefan J Schaller, Saad M Alam, Jianren Mao, Yanli Zhao, Manfred Blobner, David J Greenblatt, J A Jeevendra Martyn
OBJECTIVES: Chronic administration of morphine and midazolam, alone or in combination, can induce tolerance to their effects. Data showed that co-administration of morphine and midazolam increased effective dose requirement of morphine, exceeding that observed with morphine alone. METHODS: To elucidate the pharmacokinetic component to the tolerance, we administered midazolam (2 mg/kg) and morphine (10 mg/kg) alone or their combination daily to rats for 12 days followed by a pharmacokinetic study on day 13...
November 28, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27882602/the-resveratrol-derivatives-trans-3-5-dimethoxy-4-fluoro-4-hydroxystilbene-and-trans-2-4-5-trihydroxystilbene-decrease-oxidative-stress-and-prolong-lifespan-in-caenorhabditis-elegans
#4
Nadine Fischer, Christian Büchter, Karoline Koch, Sabrina Albert, René Csuk, Wim Wätjen
OBJECTIVES: Resveratrol (trans-3,4',5-trihydroxystilbene (1)) was previously shown to extend the lifespan of different model organisms. However, its pharmacological efficiency is controversially discussed. Therefore, the bioactivity of four newly synthesized stilbenes (trans-3,5-dimethoxy-4-fluoro-4'-hydroxystilbene (3), trans-4'-hydroxy-3,4,5-trifluorostilbene (4), trans-2,5-dimethoxy-4'-hydroxystilbene (5), trans-2,4',5-trihydroxystilbene (6)) was compared to (1) and pterostilbene (trans-3,5-dimethoxy-4'-hydroxystilbene (2)) in the established model organism Caenorhabditis elegans...
November 23, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27882565/tanshinone-iia-attenuates-a%C3%AE-25-35-induced-spatial-memory-impairment-via-upregulating-receptors-for-activated-c-kinase1-and-inhibiting-autophagy-in-hippocampus
#5
Jiejun Zhu, Shiping Liao, Liming Zhou, Lihong Wan
OBJECTIVES: Tanshinone IIA (Tan IIA) may exert significant protective effects against the neurotoxicity induced by β-amyloid protein (Aβ). This study was designed to investigate the possible neuroprotective mechanism of Tan IIA on Aβ25-35 -induced spatial memory impairment in mice. METHODS: After 3 weeks of preventive treatment (Tan IIA or oil), all male Kunming mice were subjected to Aβ25-35 (10 μl, intracerebroventricularly (i.c.v.)) to establish the spatial memory impairment model...
November 23, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27882559/lipiodol-does-not-affect-the-tissue-distribution-of-intravenous-doxorubicin-infusion-in-pigs
#6
Elsa Lilienberg, Ilse R Dubbelboer, Erik Sjögren, Hans Lennernäs
OBJECTIVES: In liver cancer treatment, lipiodol is used as a pharmaceutical excipient to improve delivery of the cytostatic drug doxorubicin (DOX). As DOX and its metabolite doxorubicinol (DOXol) cause serious off-target adverse effects, we investigated the effects of drug-free lipiodol or ciclosporin (CsA) on the tissue distribution (Kp ) of DOX and DOXol in relevant pig tissues. METHODS: Four treatment groups (TI-TIV) all received an intravenous DOX solution at 0 and 200 min...
November 23, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27859255/modulation-of-multidrug-resistance-associated-proteins-function-in-erythrocytes-in-glycerol-induced-acute-renal-failure-rats
#7
Aoi Matsushima, Keisuke Oda, Nobuhiro Mori, Teruo Murakami
OBJECTIVES: Evaluation of the function of multidrug resistance-associated proteins (MRPs) expressed in erythrocytes and screening of endogenous MRPs modulator(s) in glycerol-induced acute renal failure (ARF) rats. METHODS: Concentrations of 2,4-dinitrophenyl-S-glutathione (DNP-SG), a substrate for MRPs, in erythrocytes after administration of 1-chloro-2,4-dintrobenzene (CDNB), a precursor of DNP-SG, were determined in control and ARF rats. The screening of endogenous MRPs modulator(s) was performed using washed erythrocytes and inside-out erythrocyte membrane vesicles (IOVs) in vitro...
November 18, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27859251/a-randomized-two-way-crossover-bioequivalence-study-in-healthy-adult-volunteers-of-paediatric-zidovudine-lamivudine-nevirapine-fast-disintegrating-fixed-dose-combination-tablet
#8
Anjali Joshi, Daniel Gbadero, Fredrick Esseku, Olufikayo J Adesanya, Moji C Adeyeye
OBJECTIVE: The bioequivalence study was conducted to compare the developed paediatric fixed-dose combination (FDC) zidovudine/lamivudine/nevirapine (60/30/50 mg) tablet - the test formulation - with the combined mixture of single-entity innovator products (reference product). METHODS: A single-dose open-label randomized two-way crossover study was conducted in healthy adult African volunteers after an informed consent was obtained. The 24 volunteers, divided into two groups, were administered the products after an overnight fast on two treatment days with 14 days of washout period...
November 18, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27861887/effects-of-localized-interactions-and-surface-properties-on-stability-of-protein-based-therapeutics
#9
REVIEW
Brittney J Mills, Jennifer S Laurence Chadwick
OBJECTIVES: Protein-based therapeutics garner significant attention because of exquisite specificity and limited side effects and are now being used to accomplish targeted delivery of small-molecule drugs. This review identifies and highlights individual chemical attributes and categorizes how site-specific changes affect protein stability based on published high-resolution molecular analyses. KEY FINDINGS: Because it is challenging to determine the mechanisms by which the stability of large, complex molecules is altered and data are sparse, smaller, therapeutic proteins (insulin, erythropoietin, interferons) are examined alongside antibody data...
November 10, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27781278/improving-the-oral-bioavailability-of-buprenorphine-an-in-vivo-proof-of-concept
#10
Anand Joshi, Matthew Halquist, Zacharoula Konsoula, Yongzhen Liu, J P Jones, Christian Heidbreder, Phillip M Gerk
OBJECTIVES: The aim of this study was to improve the oral bioavailability of buprenorphine by inhibiting presystemic metabolism via the oral co-administration of 'Generally Recognized as Safe' compounds, thus providing an orally administered drug product with less variability and comparable or higher exposure compared with the sublingual route. METHODS: The present studies were performed in Sprague Dawley rats following either intravenous or oral administration of buprenorphine/naloxone and oral co-administration of 'Generally Recognized as Safe' compounds referred to as 'adjuvants'...
October 26, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27781276/effect-of-ball-milling-on-the-physicochemical-properties-of-atorvastatin-calcium-sesquihydrate-the-dissolution-kinetic-behaviours-of-milled-amorphous-solids
#11
Makiko Kobayashi, Yusuke Hattori, Tetsuo Sasaki, Makoto Otsuka
OBJECTIVES: The purposes of this study were to clarify the amorphization by ball milling of atorvastatin calcium sesquihydrate (AT) and to analyse the change in dissolution kinetics. METHODS: The amorphous AT was prepared from crystal AT by ball milling and analysed in terms of the changes of its physicochemical properties by powder X-ray diffraction analysis (XRD), thermal analysis and infrared spectroscopy (IR). Moreover, to evaluate the usefulness of the amorphous form for pharmaceutical development, intrinsic solubility of the ground product was evaluated using a dissolution kinetic method...
October 26, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27774655/phenolic-compounds-alone-or-in-combination-may-be-involved-in-propolis-effects-on-human-monocytes
#12
Eliza de Oliveira Cardoso, Bruno José Conti, Karina Basso Santiago, Fernanda Lopes Conte, Lucas Pires Garcia Oliveira, Rodrigo Tavanelli Hernandes, Marjorie de Assis Golim, José Maurício Sforcin
OBJECTIVES: Propolis is a natural product with a complex chemical composition. Its isolated compounds exert biological activities; however, its synergistic effects are unknown. The involvement of phenolic acids (caffeic - Caf, dihydrocinnamic - Cin and p-coumaric - Cou) alone or in combination was investigated in the action of propolis in human monocytes. METHODS: Cell viability was analysed by MTT assay; TNF-α, IL-6 and IL-10 production by enzyme-linked immunosorbent assay (ELISA); cell markers expression by flow cytometry; colony-forming units were counted to assess the microbicidal activity; and H2 O2 production was analysed by colorimetric assay...
October 24, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27774650/chronic-restraint-stress-increases-angiotensin-ii-potency-in-the-rat-carotid-role-of-cyclooxygenases-and-reactive-oxygen-species
#13
Hariane Côco, Larissa Pernomian, Priscila C Pereira, Mayara S Gomes, Katia C Marchi, Alexandre H Lopes, Thiago M Cunha, Carlos R Tirapelli, Ana M de Oliveira
OBJECTIVES: To investigate the mechanisms underlying the effects of chronic restraint stress on the vascular contractile response induced by angiotensin (Ang) II in rat carotid. METHODS: Concentration-response curves for AngII were obtained in endothelium-intact or endothelium-denuded carotid rings, in the absence or presence of SC-560 (COX-1 inhibitor), SC-236 (COX-2 inhibitor), wortmannin (PI3 K-Akt inhibitor), ML171 (NOX-1 inhibitor), VAS2870 (NOX-4 inhibitor), tiron (O2- scavenger) or PEG-catalase (H2 O2 scavenger)...
October 24, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27774648/phytoconstituents-as-pharmacotherapeutics-in-rheumatoid-arthritis-challenges-and-scope-of-nano-submicromedicine-in-its-effective-delivery
#14
Mahfoozur Rahman, Sarwar Beg, Amita Verma, Fahad A Al Abbasi, Firoz Anwar, Sumant Saini, Sohail Akhter, Vikas Kumar
OBJECTIVES: The present review explores the therapeutic application of herbals in rheumatoid arthritis (RA) therapy, and how nano/submicromedicine can be fit in the scope of its therapeutic delivery in RA has been addressed. KEY FINDINGS: Incorporation of bioactive such as polyphenols, thymoquinone, resveratrol, hesperidin, curcumin, celastrol and gambogic acid in a dose-dependent manner showed quite high efficacy for the treatment of RA. It can be attributed to their targeting ability against various inflammatory mediators including nitric oxide (NO), cytokines, chemokines, adhesion molecules, NF-kβ, lipoxygenase (LOXs) and arachidonic acid (AA)...
October 24, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27757958/dichloroacetate-induces-regulatory-t-cell-differentiation-and-suppresses-th17-cell-differentiation-by-pyruvate-dehydrogenase-kinase-independent-mechanism
#15
Naoyuki Makita, Jun Ishiguro, Keisuke Suzuki, Futoshi Nara
OBJECTIVES: Recently, there has been a growing interest in the mechanism of action of dichloroacetate (DCA) for T-cell differentiation; however, this mechanism has not been elucidated in detail. Therefore, this study aimed to investigate the mechanism of action of DCA for Treg and Th17 differentiation with pyruvate dehydrogenase kinase (PDHK) inhibitor (AZD7545) and PDHK knockdown. METHODS: Inhibitory activity of DCA and AZD7545 against recombinant PDHK and intracellular PDH phosphorylation was measured...
October 19, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27747875/identification-of-compounds-from-non-polar-fractions-of-blechnum-spp-and-a-multitarget-approach-involving-enzymatic-modulation-and-oxidative-stress
#16
Juliana Maria de Mello Andrade, Natasha Maurmann, Patricia Pranke, Izabel Cristina Casanova Turatti, Norberto Peporine Lopes, Amélia T Henriques
OBJECTIVES: The hexane (HEX) and dichloromethane (DCM) fractions from Blechnum binervatum, Blechnum brasiliense and Blechnum occidentale were studied about phytochemicals and biological properties using multitarget approach. METHODS: The chemical composition was performed by gas chromatography coupled with mass spectrometry detector (GC-MS) analysis. Antioxidant capacity was evaluated against free radicals and on lipid peroxidation. Monoamine oxidases (MAO) and cholinesterases enzymatic modulation, as well as effects on rat and human cells, were assessed...
October 17, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27747867/the-development-of-sustained-release-drug-delivery-platforms-using-melt-extruded-cellulose-based-polymer-blends
#17
Matthew R Wilson, David S Jones, Gavin P Andrews
OBJECTIVES: This research examined the application of hot melt extrusion (HME) in the preparation of matrix formulations containing hydroxypropyl cellulose (HPC) as a base polymer in combination with methyl cellulose (MC) and hydroxypropyl methylcellulose (HPMC). METHODS: The limit to which formulations could control drug release under varying paddle speeds, high alcohol environments and high and low drug loads was investigated on a Caleva 10 ST dissolution tester...
October 17, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27739059/palliative-medicines-for-children-a-new-frontier-in-paediatric-research
#18
Liz Jamieson, Ian C K Wong, Finella Craig, Nanna Christiansen, Karen Brombley, Catherine Tuleu, Emily Harrop
OBJECTIVES: This paper seeks to highlight from a UK perspective the current lack of a research evidence base in paediatric palliative care that has resulted in a paucity of available medicines with appropriate formulations (strength and dosage form) to provide symptom management for children with life-limiting illnesses and to raise awareness of this group of 'therapeutic orphans'. Currently, clinicians have limited, often unsuitable medication choices for their paediatric palliative care patients, with little hope of moving away from the status quo...
October 13, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27734495/nanostructured-hybrids-for-the-improvement-of-folic-acid-biopharmaceutical-properties
#19
Cinzia Pagano, Maria Cristina Tiralti, Luana Perioli
OBJECTIVES: Folic acid (FA) is an important source for the prevention of many diseases. However, its use is limited because the very low solubility (<10 mg/l particularly in the gastric environment) responsible for the incomplete adsorption of the administered dose. This study proposes a technological strategy to overcome this problem enhancing FA dissolution rate by means of a formulation able to make completely bioavailable the whole administered dose. METHODS: Folic acid was intercalated in the layered double hydroxides (LDHs) MgAl-LDH and ZnAl-LDH...
October 13, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27714817/effect-of-solvent-on-retarding-the-release-of-diltiazem-hcl-from-polyox-based-liquisolid-tablets
#20
Waseem Kaialy, Hussaini Bello, Kofi Asare-Addo, Ali Nokhodchi
OBJECTIVES: The aim of this work was to investigate the use of liquisolid technique to sustain the release of a model highly soluble drug, diltiazem HCl, from liquisolid matrices containing Polyox, a recently proposed matrix-forming hydrophilic polymer as an alternative to hypromellose. METHODS: Polyox-based liquisolid formulations prepared using several non-volatile solvents (i.e. polysorbate 80, polyethylene glycol, polyethylene glycol 200 and polyethylene glycol 600) and then characterised using differential scanning calorimetry and powder X-ray diffraction...
October 7, 2016: Journal of Pharmacy and Pharmacology
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