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Journal of Pharmacy and Pharmacology

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https://read.qxmd.com/read/30993723/alpha-linolenic-acid-ameliorates-bronchial-asthma-features-in-ovalbumin-sensitized-rats
#1
Mohammad Hossein Boskabady, Mahsa Kaveh, Farzaneh Shakeri, Nama Mohammadian Roshan, Ramin Rezaee
OBJECTIVES: Effect of alpha-linolenic acid (ALA) against ovalbumin (OVA)-induced inflammation, oxidant/antioxidant imbalance and pathological features was examined in rat. METHODS: Total and differential WBC count and oxidant/antioxidant levels in BALF (bronchoalveolar lavage fluid) as well as lung pathological features were investigated in five groups of rats including controls (group C), rats sensitized with OVA (group S) and S treated with either ALA (0.2 and 0...
April 16, 2019: Journal of Pharmacy and Pharmacology
https://read.qxmd.com/read/30989669/chlorogenic-acid-inhibits-proliferation-and-induces-apoptosis-in-a498-human-kidney-cancer-cells-via-inactivating-pi3k-akt-mtor-signalling-pathway
#2
Xiaokang Wang, Jianghong Liu, Zhanxiong Xie, Jiaoyu Rao, Gengrui Xu, Kaiyuan Huang, Wenyan Li, Zijun Yin
OBJECTIVES: Kidney cancer is a highly lethal cancer, of which the most common type is renal cell carcinoma (RCC). The targeted drugs used in treating RCC clinically have a lot of side effects. Therefore, it is urgent to find out effective agents with little toxic effects. METHODS: The antiproliferation effect of chlorogenic acid (CA) was performed using the CCK-8 assay. Then, we adopted colony formation assay, Annexin V/PI staining assay and JC-1 mitochondrial membrane potential assay to explore the mechanism of anticancer effect of CA...
April 15, 2019: Journal of Pharmacy and Pharmacology
https://read.qxmd.com/read/30957246/pitavastatin-attenuates-cisplatin-induced-renal-injury-by-targeting-mapk-and-apoptotic-pathways
#3
Swati Kaushik, Ameesha Tomar, Susrutha Puthanmadhom Narayanan, Tapas Chandra Nag, Dharamvir Singh Arya, Jagriti Bhatia
OBJECTIVE: Anti-neoplastic drug cisplatin is prescribed widely for treatment of a variety of malignancies. Its use has been restricted lately due to severe renal toxicity. The purpose of current study was to investigate the effect of pitavastatin (a hypolipidaemic drug) in cisplatin-induced acute kidney injury in rats. METHOD: Male Wistar rats (150-200 g) were treated with different doses of pitavastatin (0.16, 0.32 and 0.64 mg/kg per day p.o.; 10 days). On 7th day of the study, rats were administered cisplatin (8 mg/kg i...
April 7, 2019: Journal of Pharmacy and Pharmacology
https://read.qxmd.com/read/30919959/raloxifene-decreases-cell-viability-and-migratory-potential-in-prostate-cancer-cells-lncap-with-gpr30-gper1-involvement
#4
Giovanna Cassone Salata, Cristiane Figueiredo Pinho, André T A G de Freitas, Ariana Musa Aquino, Luis Antonio Justulin, Leonardo Oliveira Mendes, Bianca F Gonçalves, Flávia Karina Delella, Wellerson Rodrigo Scarano
OBJECTIVES: This study evaluated raloxifene (ral) effects on LNCaP prostate tumour cells modulating the activity of GPER1/GPR30 receptors. METHODS: LNCaP cells were submitted for 40/120 min and 12 h to the following treatments: C: RPMI + DMSO; R: RPMI + Ral; G: RPMI + Ral + G15 (GPER1 antagonist). Trypan blue staining measured cell viability. Migratory potential (12 h) was measured by transwell migration test in translucent inserts, which were then stained with DAPI and analysed under a fluorescence microscope for quantification...
March 28, 2019: Journal of Pharmacy and Pharmacology
https://read.qxmd.com/read/30887519/curcumin-solid-dispersion-loaded-in-situ-hydrogels-for-local-treatment-of-injured-vaginal-bacterial-infection-and-improvement-of-vaginal-wound-healing
#5
Mengmeng Zhang, Bo Zhuang, Gangjun Du, Guang Han, Yiguang Jin
OBJECTIVES: Injured vaginal infection is detrimental to women. A curcumin hydrogel was studied for local treatment of injured vaginal infection. METHODS: Curcumin solid dispersions (CSDs) were prepared from polyvinyl pyrrolidone and characterized by differential scanning calorimetry and an X-ray diffraction method. An in situ hydrogel CSD hydrogel (CSDG) was prepared with CSD/poloxamers and characterized. In vitro curcumin release and antibacterial effects of CSDs, CSDGs and curcumin were compared...
March 18, 2019: Journal of Pharmacy and Pharmacology
https://read.qxmd.com/read/30873627/a-population-pharmacokinetic-model-of-vancomycin-for-dose-individualization-based-on-serum-cystatin-c-as-a-marker-of-renal-function
#6
Tao-Tao Liu, Hui-Mei Pang, Li Jing, Wen-Xing Wei, Xiao-Ling Qin, Qing Guo, Hua Lu, Dao-Hai Cheng, Wei-Zhe Jiang
OBJECTIVES: This study aimed to establish a vancomycin population pharmacokinetics (PPK) model based on serum cystatin C and to optimize dosing for achieving targeted steady-state trough concentrations (Css ) of 10-15 and 15-20 mg/l. METHODS: Patients aged ≥18 years were prospectively enrolled. A vancomycin PPK model was built with glomerular filtration rate (GFR) as a renal covariate estimated by cystatin C. A new group of patients were used for external evaluation...
March 14, 2019: Journal of Pharmacy and Pharmacology
https://read.qxmd.com/read/30868609/tanshinone-iia-protects-against-lipopolysaccharide-induced-lung-injury-through-targeting-sirt1
#7
Minxue Quan, Yanni Lv, Yang Dai, Biying Qi, Longsheng Fu, Xuanying Chen, Yisong Qian
OBJECTIVES: This study was designed to investigate the effects and the mechanism of Tanshinone IIA (TIIA) on endotoxic shock-induced lung injury in a mouse model. METHODS: Mice were administered intraperitoneally with TIIA (10 mg/kg) 0.5 h before lipopolysaccharide (LPS) challenge and then received additional injections every 24 h during the 3-day experimental period. The physiological indexes, the survival rate and the parameters for lung injury were examined...
March 13, 2019: Journal of Pharmacy and Pharmacology
https://read.qxmd.com/read/30864160/effect-of-a-new-cyclic-derivative-of-gaba-rgpu-207-on-the-functions-of-cardiac-and-cerebral-mitochondria-of-stressed-animals
#8
Ivan Sergeevich Mokrousov, Valentina Nikolaevna Perfilova, Igor Igorevich Prokofiev, Tamara Alexandrovna Popova, Ekaterina Gennadievna Vodopyanova, Olga Sergeevna Vasil'eva, Ivan Nikolaevich Tyurenkov
OBJECTIVES: The objective of this study was to investigate the effects of a new derivative of GABA, RGPU-207 compound, on the mitochondrial functions of stressed animals. METHODS: RGPU-207 and the comparator drugs (phenibut and piracetam) were administered intraperitoneally to unstressed and stressed male rats at a dose of 9.4, 25 and 400 mg/kg, respectively. The oxygen consumption by cardiac and cerebral mitochondria in state 3 and 4 and Chance's respiratory control ratio (RCR) was investigated...
March 12, 2019: Journal of Pharmacy and Pharmacology
https://read.qxmd.com/read/30847938/mangiferin-attenuates-bleomycin-induced-pulmonary-fibrosis-in-mice-through-inhibiting-tlr4-p65-and-tgf-%C3%AE-1-smad2-3-pathway
#9
Li Jia, Ping Sun, Hui Gao, Jie Shen, Yuan Gao, Cheng Meng, Shidong Fu, Huijuan Yao, Gong Zhang
OBJECTIVES: Investigating the antipulmonary fibrosis effect of mangiferin from Mangifera indica and the possible molecular mechanism. METHODS: In vivo, bleomycin (BLM)-induced pulmonary fibrosis experimental model was used for evaluating antipulmonary fibrosis effect of mangiferin. Histopathologic examination and collagen deposition were investigated by HE and Masson staining as well as detecting the content of hydroxyproline. The expression of transforming growth factor-β1 (TGF-β1), α-smooth muscle actin (α-SMA), TLR4 and p-P65 in lung tissue was analysed through immunofluorescence...
March 7, 2019: Journal of Pharmacy and Pharmacology
https://read.qxmd.com/read/30838650/molecular-mechanism-of-tuberoinfundibular-peptide-of-39-on-glucocorticoid-receptor-mediated-glutamate-gaba-imbalance-and-cerebral-abnormalities-against-cognitive-deficit-model
#10
Gunasekaran Venkatesh, Veintramuthu Sankar, Muthiah Ramanathan
OBJECTIVES: This study is designed to evaluate the role of tuberoinfundibular peptide of 39 (TIP39) in connection with glucocorticoid receptor-mediated glutamate/GABA abnormalities in chronic unpredictable mild stress (CUMS) model. METHODS: Male Sprague-Dawley rats were treated with TIP39 (1 and 10 nmol, i.c.v) and diazepam 2 mg/kg throughout the stress period (28 days) in alternate days. Then, rats were subjected for different behavioural activity followed by biochemical, gene expression and histological examinations...
March 5, 2019: Journal of Pharmacy and Pharmacology
https://read.qxmd.com/read/30834522/synthesis-cytotoxicity-and-liver-targeting-of-3-o-%C3%AE-d-galactosylated-resveratrol
#11
Jiajia Qian, Liqiong Zha, Beilei Wang, Caiyun Zhang, Lufeng Hong, Weidong Chen
OBJECTIVES: Resveratrol (Res), a naturally occurring polyphenol, has shown pharmacological activities in treatment of liver diseases. However, the application of Res was limited by its poor bioavailability and liver targeting. Herein, 3-O-β-D-Galactosylated Resveratrol (Gal-Res) was synthesized by structural modification of Res to enhance bioavailability and liver targeting. METHODS: The Gal-Res was characterized by IR, 1 H-NMR spectra and MS. The in vitro antitumour experiments, in vivo pharmacokinetics and biodistribution studies were evaluated...
March 4, 2019: Journal of Pharmacy and Pharmacology
https://read.qxmd.com/read/30809816/endothelin-1-increases-chsy-1-expression-in-aortic-endothelial-cells-via-transactivation-of-transforming-growth-factor-%C3%AE-type-i-receptor-induced-by-type-b-receptor-endothelin-1
#12
Faezeh Seif, Peter J Little, Reyhaneh Niayesh-Mehr, Masoumeh Zamanpour, Hossein Babaahmadi-Rezaei
OBJECTIVES: TGF-β through hyperelongation of glycosaminoglycan (GAG) chains leads to binding of low-density lipoproteins to the proteoglycans. The vasoactive peptide, endothelin-1 (ET-1), plays a key role in the development of atherosclerosis. This study addressed the question whether ET-1 by activating the Rho kinase and cytoskeletal rearrangement can transactivate the TGF-β receptor leading to phosphorylation of the transcription factor Smad2 and increased expression of the GAG chain synthesizing enzyme such as chondroitin synthase-1 (CHSY-1) in bovine aortic endothelial cells (BAECs)...
February 27, 2019: Journal of Pharmacy and Pharmacology
https://read.qxmd.com/read/30809806/neuroprotective-effect-of-pharmacological-postconditioning-on-cerebral-ischaemia-reperfusion-induced-injury-in-mice
#13
Amarjot Kaur Grewal, Nirmal Singh, Thakur Gurjeet Singh
OBJECTIVES: To investigate the mechanism of neuroprotection rendered via pharmacological postconditioning in cerebral ischaemia-reperfusion-induced injury in mice. METHODS: Pharmacological postconditioning is strategy which either involves hindering deleterious pathway or inducing modest stress level which triggers intracellular defence pathway to sustain more vigorous insult leading to conditioning. Hence, in current research we explored the potentiality of CGS21680 (0...
February 27, 2019: Journal of Pharmacy and Pharmacology
https://read.qxmd.com/read/30805935/easy-and-effective-method-to-generate-endotoxin-free-chitosan-particles-for-immunotoxicology-and-immunopharmacology-studies
#14
Filipa Lebre, Ed C Lavelle, Olga Borges
OBJECTIVES: The cationic biopolymer chitosan (CH) has emerged as a promising candidate adjuvant due to its safety profile and immunostimulatory properties. The presence of endotoxin contamination in biomaterials is generally underappreciated and can generate misleading results. It is important to establish a convenient methodology to obtain large amounts of high quality chitosan nanoparticles for biomedical applications. METHODS: We developed an easy method to generate endotoxin-free chitosan and assessed its purity using the Limulus amebocyte lysate assay and by measuring dendritic cell activation...
February 25, 2019: Journal of Pharmacy and Pharmacology
https://read.qxmd.com/read/30793317/application-of-the-relationship-between-pharmacokinetics-and-pharmacodynamics-in-drug-development-and-therapeutic-equivalence-a-pearrl-review
#15
REVIEW
Ioannis Loisios-Konstantinidis, Rafael L M Paraiso, Nikoletta Fotaki, Mark McAllister, Rodrigo Cristofoletti, Jennifer Dressman
OBJECTIVES: The objective of this review was to provide an overview of pharmacokinetic/pharmacodynamic (PK/PD) models, focusing on drug-specific PK/PD models and highlighting their value added in drug development and regulatory decision-making. KEY FINDINGS: Many PK/PD models, with varying degrees of complexity and physiological understanding have been developed to evaluate the safety and efficacy of drug products. In special populations (e.g. paediatrics), in cases where there is genetic polymorphism and in other instances where therapeutic outcomes are not well described solely by PK metrics, the implementation of PK/PD models is crucial to assure the desired clinical outcome...
February 22, 2019: Journal of Pharmacy and Pharmacology
https://read.qxmd.com/read/30793320/prolonged-therapy-with-the-anticonvulsant-carbamazepine-leads-to-increased-plasma-clearance-of-fentanyl
#16
Ala Nozari, Oluwaseun Akeju, Hooman Mirzakhani, Emad Eskandar, Zhijun Ma, Md Amin Hossain, Qingping Wang, David J Greenblatt, J A Jeevendra Martyn
OBJECTIVES: Fentanyl is a potent analgesic that accounts for an increasing number of overdose deaths in the United States. This study tested whether altered pharmacokinetics plays a pivotal role in the increased fentanyl dose requirements in patients receiving the enzyme-inducing anticonvulsant, carbamazepine. METHODS: Neurosurgical patients receiving carbamazepine for >6 weeks (N = 11) or no carbamazepine (N = 6, controls) received a single bolus dose of fentanyl (200 μg) intravenously...
February 21, 2019: Journal of Pharmacy and Pharmacology
https://read.qxmd.com/read/30793315/abyssinone-v-a-prenylated-flavonoid-isolated-from-the-stem-bark-of-erythrina-melanacantha-increases-oxidative-stress-and-decreases-stress-resistance-in-caenorhabditis-elegans
#17
Karoline Koch, Gabriel Schulz, Wera Döring, Christian Büchter, Susannah Havermann, Patrick Chalo Mutiso, Claus Passreiter, Wim Wätjen
OBJECTIVES: Recent studies showed that distinct extracts of Erythrina species used in the traditional medicine of sub-Saharan Africa are protective against stress conditions. However, the underlying molecular mechanisms as well as relevant compounds remain unclear. METHODS: We used the model organism Caenorhabditis elegans to investigate compounds isolated from the stem bark of Erythrina melanacantha (abyssinone V (1), abyssinon-4'O-methylether (2), sigmoidin B-4'O-methylether (3), glabranin (4), 8-prenylnaringenin (5), citflavanone (6), exiguaflavanone (7) and homoeriodictyol (8))...
February 21, 2019: Journal of Pharmacy and Pharmacology
https://read.qxmd.com/read/30784086/high-throughput-screening-of-excipients-with-a-biological-effect-a-kinetic-study-on-the-effects-of-surfactants-on-efflux-mediated-transport
#18
John Pollard, Ali Rajabi-Siahboomi, Raj K S Badhan, Afzal R Mohammed, Yvonne Perrie
OBJECTIVE: In this study, we develop and apply a high-throughput screening protocol to investigate the activity of non-ionic surfactants, with a broad range of hydrophilic-lipophilic balance values, against ABCB1-mediated efflux transport and ABCC2-mediated efflux transport. METHODS: Caco-2 cells were grown for 7 days in 96-well plates, then washed and incubated with the test materials for 2 h in the presence of 2.5 μm of either rhodamine 123 (R-123) or 5(6)-Carboxy-2',7' dichlorofluorescein diacetate as probes of ABCB1 and ABCC2, respectively...
February 19, 2019: Journal of Pharmacy and Pharmacology
https://read.qxmd.com/read/30784084/the-preparation-and-investigation-of-spinosin-phospholipid-complex-self-microemulsifying-drug-delivery-system-based-on-the-absorption-characteristics-of-spinosin
#19
Panpan Song, Changjiangsheng Lai, Junbo Xie, Yanqing Zhang
OBJECTIVES: The aim of this research was to investigate the intestinal absorption characteristics and mechanisms of spinosin (SPI), and a new dosage form was prepared to increase the intestinal absorption of SPI. METHODS: In this study, the intestinal absorption characteristics and mechanisms of SPI were first investigated using in situ absorption model and Caco-2 monolayer model. Subsequently, the phospholipid complex (PLC) loaded with SPI was prepared followed by a self-microemulsifying drug delivery system (SMEDDS) technique for developing a more efficient formulation...
February 19, 2019: Journal of Pharmacy and Pharmacology
https://read.qxmd.com/read/30784067/intra-articular-mucilages-behavioural-and-histological-evaluations-for-a-new-model-of-articular-pain
#20
Laura Micheli, Carla Ghelardini, Elena Lucarini, Carmen Parisio, Elena Trallori, Lorenzo Cinci, Lorenzo Di Cesare Mannelli
OBJECTIVES: The creation of a new valid preclinical model of articular pain by the intra-articular (i.a.) injection of mucilages for the screening of new treatments against arthritis. METHODS: A single intra-articular injection (20 μl) of mucilages (from Althaea officinalis roots and Linum usitatissimun seeds) or vegetal components (Amorphophallus konjac gum powder and β-glucan, used as reference standard) were assessed in the rat. The pathology progression was monitored by behavioural measurements (paw pressure test, von Frey test, incapacitance test and beam balance test) and compared to that induced by the i...
February 19, 2019: Journal of Pharmacy and Pharmacology
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