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Journal of Pharmacy and Pharmacology

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https://www.readbyqxmd.com/read/28321889/antihyperglycaemic-activity-of-the-methanol-extract-from-leaves-of-eremophila-maculata-scrophulariaceae-in-streptozotocin-induced-diabetic-rats
#1
Fadia S Youssef, Mohamed L Ashour, Sherif S Ebada, Mansour Sobeh, Hesham A El-Beshbishy, Abdel Nasser Singab, Michael Wink
OBJECTIVES: This study was designed to evaluate the antihyperglycaemic activity of the methanol leaf extract of Eremophila maculata (EMM) both in vitro and in vivo. METHODS: The antihyperglycaemic activity was assessed in vitro using differentiated 3T3-L1 adipocytes, whereas in-vivo effect was evaluated in streptozotocin-induced diabetic rats. Chemical profiling of EMM was done using LC-ESI-MS techniques. Molecular modelling experiments of the identified compounds were performed using C-Docker protocol...
March 21, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28317117/comparative-pharmacokinetic-evaluation-of-lopinavir-and-lopinavir-loaded-solid-lipid-nanoparticles-in-hepatic-impaired-rat-model
#2
Punna Rao Ravi, Rahul Vats
OBJECTIVE: Drug-induced hepatotoxicity is a major cause of concern in patients receiving HIV/TB co-treatment. Lopinavir (LPV), an anti-HIV drug, shows poor plasma exposure due to hepatic first-pass metabolism. In this study, we investigated the effect of hepatotoxicity on pharmacokinetics of free LPV and LPV-loaded solid lipid nanoparticles (LPV SLNs) in male Wistar rats. METHODS: Hepatic impairment model in rats was developed by injecting CCl4 (i.p., 2 ml/kg). Comparative pharmacokinetic (n = 5) and tissue distribution studies (n = 3) were conducted following oral administration (20 mg/kg) of free LPV and LPV SLNs in normal and hepatic impaired rats...
March 19, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28299800/the-formation-of-a-host-guest-inclusion-complex-system-between-%C3%AE-cyclodextrin-and-baicalin-and-its-dissolution-characteristics
#3
Jing Li, Qihua Jiang, Ping Deng, Qian Chen, Mingan Yu, Jingchuan Shang, Wei Li
OBJECTIVES: Baicalin (BCL) has potential therapeutic benefits, but its clinical outcomes are restricted mainly because of low water solubility. This study sought to improve the water solubility of BCL by the formation of inclusion complex with β-cyclodextrin (β-CD). METHODS: The inclusion complex was studied by solubility test, differential scanning calorimeter (DSC), Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), (1) H Nuclear magnetic resonance ((1) HNMR) and scanning electron microscopy (SEM)...
March 16, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28295319/preparation-pharmacokinetics-and-tumour-suppressive-activity-of-berberine-liposomes
#4
Xinghui Wang, Qiong Wang, Zhihui Liu, Xiao Zheng
OBJECTIVES: Berberine (BBR) has shown promising antitumour effects in vitro. However, intravenous administration of BBR solution is complicated by lethal adverse cardiovascular effects. The aim of this study was to prepare common and polyethylene glycol (PEG)-modified long-circulating BBR liposomes and evaluate their efficacy and safety as potential antitumour agents. METHODS: Physiochemical properties of common and long-circulating BBR liposomes were characterized including particle size, Zeta potential and thermal stability...
March 15, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28294340/neuroprotective-effects-of-artemisinin-against-isoflurane-induced-cognitive-impairments-and-neuronal-cell-death-involve-jnk-erk1-2-signalling-and-improved-hippocampal-histone-acetylation-in-neonatal-rats
#5
Guang Xu, Yun-Li Huang, Ping-le Li, Hai-Ming Guo, Xue-Ping Han
OBJECTIVE: This study was performed to assess the effect of artemisinin against isoflurane-induced neuronal apoptosis and cognitive impairment in neonatal rats. METHODS: Artemisinin (50, 100 or 200 mg/kg b.wt/day; oral gavage) was administered to separate groups of neonatal rats starting from postnatal day 3 (P3) to postnatal day 21 (P21). On postnatal day 7 (P7), animals were exposed to inhalation anaesthetic isoflurane (0.75%) for 6 h. KEY FINDINGS: Neuronal apoptosis following anaesthetic exposure was significantly reduced by artemisinin...
March 12, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28294333/permeation-characteristics-of-hypericin-across-caco-2-monolayers-in-the-presence-of-single-flavonoids-defined-flavonoid-mixtures-or-hypericum-extract-matrix
#6
Sheela Verjee, Olaf Kelber, Christiane Kolb, Heba Abdel-Aziz, Veronika Butterweck
OBJECTIVES: The major aim of this study was to get a detailed understanding of the exposure and fate of hypericin in the Caco-2 cell system when combined with various flavonoids, mixtures of flavonoids or Hypericum perforatum extract matrix (STW3-VI). METHODS: The permeation characteristics of hypericin in the absence or presence of quercetin, quercitrin, isoquercitrin, hyperoside and rutin were tested. Hypericin (5 μm) was mixed with single flavonoids (20 μm) or with different flavonoid combinations (each flavonoid 4 or 10 μm, total flavonoid concentration: 20 μm)...
March 12, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28295316/inhibition-of-pro-inflammatory-mediators-in-raw264-7-cells-by-7-hydroxyflavone-and-7-8-dihydroxyflavone
#7
Zhen Jin, Yao-Zhi Yang, Jian-Xin Chen, You-Zhi Tang
OBJECTIVES: Flavonoids are a class of compounds that having the benzo-γ-pyrone skeleton, which possess anti-inflammatory properties in vitro and in vivo. The aim of this study was to investigate the inhibition of two flavonoids 7-hydroxyflavone (HF) and 7,8-dihydroxyflavone (DHF) on the production of pro-inflammatory mediators in RAW264.7 cells activated by lipopolysaccharides (LPS). METHODS: For this purpose, we selected four pro-inflammatory mediators including nitric oxide (NO), prostaglandin E2 (PGE2 ), tumour necrosis factor-α (TNF-α) and interleukin-6 (IL-6) as markers to evaluate the anti-inflammatory activity of HF and DHF...
March 10, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28271502/trigonelline-and-vildagliptin-antidiabetic-effect-improvement-of-insulin-signalling-pathway
#8
Amat-Alrazaq A Aldakinah, Muhammad Y Al-Shorbagy, Dalaal M Abdallah, Hanan S El-Abhar
OBJECTIVES: Trigonelline (TRG) is known to have an antidiabetic efficacy; however, its mechanism is not entirely elucidated. METHODS: Hence, its effect on insulin signaling, besides its effectiveness in combination with vildagliptin (VLD) in a Type 2 diabetes model has been tested. KEY FINDINGS: TRG (50 mg/kg; p.o) lowered serum glucose, fructosamine, insulin, and HOMA-IR index and increased insulin sensitivity in soleus muscle via augmenting insulin receptor autophosphorylation (IR-PH), pT308-Akt, and glucose transporter 4 (GLUT4)...
March 8, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28271498/statins-anticancer-targeted-delivery-systems-re-purposing-an-old-molecule
#9
REVIEW
Sally Safwat, Rania A Ishak, Rania M Hathout, Nahed D Mortada
OBJECTIVES: Exploring the use of statins as anticancer agents and exploiting different drug delivery systems in targeting these molecules to cancerous sites. Literature review was performed to investigate the use of statins in cancer treatment in one hand, and the different pharmaceutical approaches to deliver and target these drugs to their site of action. KEY FINDINGS: Statins were used for decades as antihypercholestrolemic drugs but recently have been proven potential for broad anticancer activities...
March 8, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28271494/characterization-of-anti-inflammatory-effect-and-possible-mechanism-of-action-of-tibouchina-granulosa
#10
Andrea P Sobrinho, Alan S Minho, Leide L C Ferreira, Gabriel R Martins, Fabio Boylan, Patricia D Fernandes
OBJECTIVES: Tibouchina granulosa, popularly known as 'quaresmeira', belong to a genus widely used in the traditional medicine as infusions from their leaves. Other species of Tibouchina are used as antibacterial, antioxidant or antileishmanial. In this work, our objectives were to investigate the biological effects of T. granulosa in models of acute inflammation. METHODS: Chemical analysis showed the presence of proanthocyanidins and flavonoids. Infusions from leaves of T...
March 8, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28266713/personalised-dosing-of-medicines-for-children
#11
REVIEW
Basma Al-Metwali, Hussain Mulla
OBJECTIVES: Doses for most drugs are determined from population-level information, resulting in a standard ?one-size-fits-all' dose range for all individuals. This review explores how doses can be personalised through the use of the individuals' pharmacokinetic (PK)-pharmacodynamic (PD) profile, its particular application in children, and therapy areas where such approaches have made inroads. KEY FINDINGS: The Bayesian forecasting approach, based on population PK/PD models that account for variability in exposure and response, is a potent method for personalising drug therapy...
March 7, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28266029/decorin-loaded-poly-lactic-co-glycolic-acid-nanoparticles-modified-by-anti-alpha-fetoprotein-antibody-preparation-proliferation-inhibition-and-induced-apoptosis-effects-on-hepg2-cells-in-vitro
#12
Qiaoli Yang, Shuyue Wang, Yuan Wang, Yane Qu, Jun Xue, Yang Mi, Yanhong Wang, Xuguang Luo, Zhihua Deng, Guiqin Wang
OBJECTIVES: Decorin (DCN) is a negative regulatory factor for the growth of cancer cells and can inhibit the proliferation, metastasis of cancer cells and angiogenesis in cancer tissues. The aims of this study were to prepare the nanoparticles consisting of DCN and poly lactic-co-glycolic acid (PLGA) modified by anti-alpha fetoprotein (AFP) monoclonal antibody (mAb) and to examine the conventional physical properties, the in-vitro release of DCN and the targeting effect of these nanoparticles on HepG2 cells...
March 7, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28266023/astragaloside-ii-sensitizes-human-hepatocellular-carcinoma-cells-to-5-fluorouracil-via-suppression-of-autophagy
#13
Meng Wang, Can Huang, Yong Su, Cui Yang, Quan Xia, Du-Juan Xu
OBJECTIVES: Inhibition of autophagy has been increasingly recognized as a potential therapeutic approach against cancer. Our previous reports showed that Astragaloside II improves hepatic cancer cells resistance by downregulating MDR1 and P-gp .The purpose of this study was to further investigated the effect of autophagy on AS-II reversing multidrug resistance and its molecular mechanism in hepatocellular carcinoma cells in vitro. METHODS: Bel-7402 and Bel-7402/FU cell lines were used in this study...
March 7, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28266019/quality-control-of-hypericum-perforatum-l-analytical-challenges-and-recent-progress
#14
REVIEW
Anastasia Agapouda, Anthony Booker, Tivadar Kiss, Judit Hohmann, Michael Heinrich, Dezső Csupor
OBJECTIVES: The most widely applied qualitative and quantitative analytical methods in the quality control of Hypericum perforatum extracts will be reviewed, including routine analytical tools and most modern approaches. KEY FINDINGS: Biologically active components of H. perforatum are chemically diverse; therefore, different chromatographic and detection methods are required for the comprehensive analysis of St. John's wort extracts. Naphthodianthrones, phloroglucinols and flavonoids are the most widely analysed metabolites of this plant...
March 7, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28266011/traditional-uses-phytochemistry-and-pharmacology-of-the-medicinal-species-of-the-genus-cordia-boraginaceae
#15
REVIEW
Manisha J Oza, Yogesh A Kulkarni
OBJECTIVES: Cordia (family Boraginaceae) is a genus of deciduous flowering trees or shrubs comprising more than 300 species distributed widely in the tropical regions. The aim of this review was to provide exhaustive scientific information on traditional uses, phytochemistry and pharmacological activities of the 36 important species with medicinal value from the genus Cordia, to divulge prospects for further research on its therapeutic potential. KEY FINDINGS: Leaves, fruit, bark and seed of a majority of the species were found to possess abundant ethnomedicinal value, but leaves were found to be used most frequently to treat many ailments such as respiratory disorders, stomach pain, wound, inflammation, myalgia, cough, dysentery and diarrhoea...
March 7, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28220495/influence-of-hyperglycemia-on-liver-inflammatory-conditions-in-the-early-phase-of-non-alcoholic-fatty-liver-disease-in-mice
#16
Shinichi Harada, Kei Miyagi, Tokio Obata, Yasuko Morimoto, Kazuo Nakamoto, Ke Ih Kim, Soo Ki Kim, Soo Ryang Kim, Shogo Tokuyama
OBJECTIVES: A non-alcoholic fatty liver disease (NAFLD) has high prevalence and now important issue of public health. In general, there exists strong interaction between NAFLD and diabetes, but the detailed mechanism is unclear. In this study, we determined the effects of hyperglycemia on progression in the early phase of NAFLD in mice. METHODS: Male ddY mice were fed a choline-deficient, l-amino acid-defined, high-fat diet (CDAHFD) consisting of 60% of kcal from fat and 0...
February 21, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28220483/pharmacokinetics-and-pharmacodynamics-of-metamizol-in-co-administration-with-morphine-under-acute-and-chronic-treatments-in-arthritic-rats
#17
Patricia Esmeralda Carrillo-Calzadilla, Francisco Javier López-Muñoz, Luis Alfonso Moreno-Rocha, José Raúl Medina-López, Alma Rosa Cortés-Arroyo, Adriana Miriam Domínguez-Ramírez
OBJECTIVE: To investigate the relationship between metamizol pharmacokinetics and the antinociceptive effect produced after subcutaneous administration of metamizol (177.8 mg/kg) alone or in combination with morphine (3.2 mg/kg), under acute and chronic treatments. METHODS: Antinociception was assessed using the pain-induced functional impairment model in rat (PIFIR). Serial blood samples were collected from the same animals to study the pharmacokinetics of metamizol...
February 21, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28211640/complexation-of-oxethazaine-with-2-hydroxypropyl-%C3%AE-cyclodextrin-increased-drug-solubility-decreased-cytotoxicity-and-analgesia-at-inflamed-tissues
#18
Andressa R Prado, Fabiano Yokaichiya, Margareth Kazuyo Kobayashi Dias Franco, Camila Morais Gonçalves da Silva, Laura Oliveira-Nascimento, Michelle Franz-Montan, Maria C Volpato, Luís F Cabeça, Eneida de Paula
OBJECTIVES: Oxethazaine (OXZ) is one of the few local anaesthetics that provides analgesia at low pH, but presents poor solubility, cytotoxicity and no parenteral formulations. To address these issues, we aimed to prepare OXZ host-guest inclusion complex with hydroxypropyl-beta-cyclodextrin (HP-β-CD). METHODS: The inclusion complex was formed by co-solubilization, followed by a job plot analysis to determine stoichiometry of complexation and dialysis equilibrium analysis (based on UV/VIS absorption and fluorescence profiles of OXZ)...
February 17, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28211580/inhibition-of-pde5a1-guanosine-cyclic-monophosphate-cgmp-hydrolysing-activity-by-sildenafil-analogues-that-inhibit-cellular-cgmp-efflux
#19
Anna Subbotina, Aina W Ravna, Roy A Lysaa, Ruben Abagyan, Ryszard Bugno, Georg Sager
OBJECTIVES: To determine the ability of 11 sildenafil analogues to discriminate between cyclic nucleotide phosphodiesterases (cnPDEs) and to characterise their inhibitory potencies (Ki values) of PDE5A1-dependent guanosine cyclic monophosphate (cGMP) hydrolysis. METHODS: Sildenafil analogues were identified by virtual ligand screening (VLS) and screened for their ability to inhibit adenosine cyclic monophosphate (cAMP) hydrolysis by PDE1A1, PDE1B1, PDE2A1, PDE3A, PDE10A1 and PDE10A2, and cGMP hydrolysis by PDE5A, PDE6C, PDE9A2 for a low (1 nm) and high concentration (10 μm)...
February 17, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28211571/inhibitory-effects-of-a-standardized-extract-of-justicia-pectoralis-in-an-experimental-rat-model-of-airway-hyper-responsiveness
#20
Carlos T M Moura, Francisco J Batista-Lima, Teresinha S Brito, Alfredo A V Silva, Luan C Ferreira, Cássia R Roque, Karoline S Aragão, Alexandre Havt, Francisco N Fonseca, Luzia K A M Leal, Pedro J C Magalhães
OBJECTIVE: Justicia pectoralis is a plant useful for the treatment of respiratory diseases. Here, we studied the antiasthmatic properties of a standardized extract of J. pectoralis (Jp). METHODS: Ovalbumin (OVA)-sensitized rats were actively challenged with saline or OVA to study airway hyper-responsiveness after oral treatment with saline or Jp. The ability of Jp to inhibit hyper-reactivity was evaluated in isolated trachea mounted in isolated organ bath chamber...
February 17, 2017: Journal of Pharmacy and Pharmacology
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