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Journal of Pharmacy and Pharmacology

Ya-Jun Li, Lin Wang, Bei Zhang, Fei Gao, Chun-Mei Yang
OBJECTIVES: It has been proven that extracellular HMGB1 is involved in progression of neurologic disorders, such as stroke, traumatic brain injury, meningitis and epilepsy. Glycyrrhizin (GL) is a direct inhibitor of HMGB1, and blocks HMGB1 release into the extracellular. We aim in this study to investigate the neuroprotective effects of GL in a rat model after lithium-pilocarpine-induced status epilepticus (SE). METHODS: Adult male SD rats were divided into three groups: Sham group, SE-group and (SE + GL)-treated group...
November 12, 2018: Journal of Pharmacy and Pharmacology
Yu-Si Cheng, Jie Chao, Chen Chen, Lin-Li Lv, Yu-Chen Han, Bi-Cheng Liu
OBJECTIVES: Oxidative stress plays a critical role in the pathogenesis of diabetic nephropathy (DN). p66shc is closely related to oxidative stress. However, the exact mechanism of its involvement in diabetic nephropathy is poorly understood. This study aimed to investigate the role of the p66shc-related pathway in diabetic nephropathy. METHODS: In an in-vivo experiment, rats were injected with streptozotocin to induce early diabetic nephropathy. The treatment groups were an aminoguanidine group and an enzastaurin group...
November 12, 2018: Journal of Pharmacy and Pharmacology
Bahar Matin, Ahmad A Sherbini, Novera Alam, Jerold S Harmatz, David J Greenblatt
OBJECTIVES: Resveratrol is a naturally occurring antioxidant with therapeutic potential in prevention and treatment of neoplastic disease and other human disorders. However, net clearance of resveratrol in humans is very high, mainly due to glucuronide conjugation. This leads to extensive presystemic extraction and low plasma concentrations after oral dosage. The present study evaluated the effect of probenecid, an inhibitor of glucuronide conjugation, on resveratrol metabolism in vitro...
November 12, 2018: Journal of Pharmacy and Pharmacology
Michaela Eisenhardt, Peggy Schlupp, Frank Höfer, Thomas Schmidts, Daniel Hoffmann, Peter Czermak, Anne-Kathrin Pöppel, Andreas Vilcinskas, Frank Runkel
OBJECTIVES: The objective of this study was to investigate the therapeutic potential of the insect metalloproteinase inhibitor (IMPI) from Galleria mellonella, the only known specific inhibitor of M4 metalloproteinases. METHODS: The fusion protein IMPI-GST (glutathione-S-transferase) was produced by fermentation in Escherichia coli and was tested for its ability to inhibit the proteolytic activity of the M4 metalloproteinases thermolysin and Pseudomonas elastase (PE), the latter a key virulence factor of the wound-associated and antibiotic-resistant pathogen Pseudomonas aeruginosa...
November 8, 2018: Journal of Pharmacy and Pharmacology
Shimaa M Ashmawy, Sanaa A El-Gizawy, Gamal M El Maghraby, Mohamed A Osman
OBJECTIVES: The aim of this research was to assess regional difference in the intestinal absorption of ranitidine HCl as an indicator for the potential effect of P-glycoprotein (P-gp) efflux transporters. METHODS: In situ rabbit intestinal perfusion was used to investigate absorption of ranitidine HCl, a substrate for P-gp efflux from duodenum, jejunum, ileum and colon. This was conducted both in the presence and absence of piperine as P-gp inhibitor. KEY FINDINGS: Ranitidine HCl was incompletely absorbed from rabbit intestine...
October 26, 2018: Journal of Pharmacy and Pharmacology
Adel A Gomaa, Dalia A El-Sers, Nahla I Al-Zokeim, Mohamed A Gomaa
OBJECTIVES: To determine the efficacy of Corchorus olitorius (C. olitorius) leaf extract in the prevention of metabolic syndrome induced in rats by high-fat diet (HFD) and compare it with that of orlistat. METHODS: Phytochemical analysis was performed. Effect of orlistat and C. olitorius extract on lipase activity and acute food intake were investigated. Body weight, biochemical parameters and histopathological examination were demonstrated. KEY FINDINGS: Corchorus olitorius extract inhibited the pancreatic lipase activity, but orlistat was more potent...
October 26, 2018: Journal of Pharmacy and Pharmacology
Takuya Matsui, Chihiro Ito, Ayumi Kato, Tian-Shung Wu, Masataka Itoigawa
OBJECTIVES: We investigated the apoptotic activities of acrofolione A (1) and B (2) isolated from Acronychia pedunculata against a human pre-B cell leukaemia cell line (NALM-6) to explore the apoptosis-related signalling molecules targeted by 1 and 2. METHODS: The apoptosis effects of 1 and 2 in NALM-6 cells were investigated by TUNEL staining, annexin V, mitochondria membrane potential and caspase 3/7 activity. We carried out a protein array to explore the signalling molecules involved in apoptosis comprehensively...
October 25, 2018: Journal of Pharmacy and Pharmacology
Angela Verma, Yau-Min Lam, Yun-Chung Leung, Xiaohui Hu, Xin Chen, Edwin Cheung, Kin Yip Tam
OBJECTIVES: Drug combination in cancer therapy aims to achieve synergistic therapeutic effect, reduced drug dosage, reduced drug toxicity and minimizes or delays the induction of drug resistance. In the present study, we investigated the anticancer effects of the combination of two metabolic modulators, dichloroacetate (DCA) and bacillus caldovelox arginase (BCA) (or pegyated human arginase (HA)). METHODS: The combination treatments were evaluated in MCF-7 and MDA-MB 231 cells as well as in MDA-MB 231 breast cancer xenograft model...
October 25, 2018: Journal of Pharmacy and Pharmacology
Erinaldo Ubirajara Damasceno Dos Santos, Tiago F Sampaio, Aléxia D Tenório Dos Santos, Fernanda C Bezerra Leite, Ronaldo C da Silva, Sergio Crovella, Amdore Guescel C Asano, Nadja Maria Jorge Asano, Paulo Roberto E de Souza
OBJECTIVES: The aim of this study was to evaluate a possible relationship between DRD2/ANKK1 (rs1800497) and SLC6A3/DAT1 (rs28363170) gene polymorphisms with the response to levodopa (L-DOPA)-therapy in patients with Parkinson's disease (PD). METHODS: One hundred and ninety-five patients with idiopathic PD were investigated. Patients were genotyped for rs1800497 and rs28363170 polymorphisms using PCR-RFLP. Logistic regression was performed to assess the association of polymorphisms with the occurrence of the chronic complications of L-DOPA therapy...
October 23, 2018: Journal of Pharmacy and Pharmacology
Jiake He, Ge Zhang, Qiuyang Zhang, Jiayin Chen, Yongjie Zhang, Xiaoxia An, Pan Wang, Shan Xie, Fang Fang, Jianheng Zheng, Yue Tang, Jiabi Zhu, Yang Yu, Xijing Chen, Yang Lu
OBJECTIVES: The present study was designed to assess the pharmacokinetic and pharmacodynamic performance of inhaled recombinant human insulin (rh-insulin) dry powders together with their safety profiles after 14-day inhalation. METHODS: In the pharmacokinetic and pharmacodynamic study, pulmonary surfactant (PS)-loaded and phospholipid hexadecanol tyloxapol (PHT)-loaded rh-insulin dry powders were intratracheally administered to male rats at the dose of 20 U/kg...
October 15, 2018: Journal of Pharmacy and Pharmacology
Irina Ielciu, Ange Mouithys-Mickalad, Thierry Franck, Luc Angenot, Allison Ledoux, Ramona Păltinean, Ewa Cieckiewicz, Delphine Etienne, Monique Tits, Gianina Crişan, Michel Frédérich
OBJECTIVES: The aim of the present study consisted in the isolation of flavonoids from the leaves of Bryonia alba L. and evaluation of their antioxidant activity and inhibition on peroxidase-catalysed reactions. METHODS: Flavonoids were isolated by preparative HPLC-DAD and their structures were elucidated by MS and NMR. Inhibitory effect was tested by the horseradish peroxidase and the myeloperoxidase assays. Cellular antioxidant assays consisted in testing the inhibitory activity on the reactive oxygen species released upon activation of neutrophils freshly isolated ex vivo from equine blood and of human monocytes-derived macrophages in vitro...
October 15, 2018: Journal of Pharmacy and Pharmacology
Masashi Kawami, Natsuko Honda, Mioka Miyamoto, Ryoko Yumoto, Mikihisa Takano
OBJECTIVES: We had previously found that reduced folate carrier (RFC; SLC19A1) is mainly involved in an influx of transport of methotrexate (MTX), a folate analogue, using alveolar epithelial A549 cells. Therefore, we examined MTX uptake in NCl-H441 (H441) cells, another in vitro alveolar epithelial model, focusing on the localization of RFC in the present study. METHODS: Transport function of RFC in H441 cells was studied using [3 H]MTX. KEY FINDINGS: The uptake of MTX was increased remarkably after pretreatment of the cell monolayer with ethylenediaminetetraacetic acid (EDTA) in H441 cells but not in A549 cells, indicating the contribution of the basolaterally located transporter...
October 15, 2018: Journal of Pharmacy and Pharmacology
Qian-Wen Yang, Qiao Li, Jie Zhang, Qian Xu, Xin Yang, Zhi-Yong Li, Hui Xu
OBJECTIVES: Andrographlide sulphonate E, namely sodium 9-dehydro-17-hydro-andrographolide-19-yl sulphate, was one of the major ingredients of Xiyanping injection. The present study aimed to demonstrate its suitability as a reference standard for use of quality control of this traditional Chinese medicine preparation made from andrographlide that has been widely used to treat various infectious diseases. METHODS: The stable crystals were prepared for unambiguous elucidation of the chemical structure by comprehensive spectral and thermal analysis...
October 15, 2018: Journal of Pharmacy and Pharmacology
Vivek B Mathema, Wanna Chaijaroenkul, Kesara Na-Bangchang
OBJECTIVES: To evaluate the cytotoxic activity of atractylodin and its potential effects on heme oxygenase (HO)-1 production, STAT1/3 phosporylation and major NF-κB protein expression in the cholangiocarcinoma-associated cell line CL-6. METHODS: Standard MTT assay was used for accessing antiproliferative activity on CL-6 cells. Normal human embryonic fibroblast (OUMS) cell was taken as control cell line. Colony formation and wound healing assay were conducted to access the effects of atractylodin on cell proliferation and directional migration activity of CL-6 cells...
October 15, 2018: Journal of Pharmacy and Pharmacology
Gokhan Zengin, Eulogio J Llorent-Martínez, Lucía Molina-García, María Luisa Fernández-de Córdova, Abdurrahman Aktumsek, Sengul Uysal, Kannan R R Rengasamy, Muhammad Zakariyyah Aumeeruddy, Mir Babak Bahadori, Mohamad Fawzi Mahomoodally
OBJECTIVES: This study investigates into the biological effects of solvent extracts (ethyl acetate, methanol, and water) of Scutellaria orientalis L. and Scutellaria salviifolia Benth. based on its enzyme inhibitory activity and antioxidant ability together with the screening of bioactive compounds. METHODS: Total and individual bioactive components were determined using spectrophotometric and HPLC-ESI-MS methods. Six antioxidant assays were conducted and enzyme inhibition was tested against key enzymes linked to the pathology of common chronic disorders...
October 10, 2018: Journal of Pharmacy and Pharmacology
Douglas Costa Gontijo, Geraldo Célio Brandão, Maria Fernanda Alves do Nascimento, Alaíde Braga de Oliveira
OBJECTIVES: To assess the antiplasmodial activity of the ethanol extract of Xylopia sericea leaves, Annonaceae, often associated with antimalarial use and to perform a bioguided isolation of active compounds. METHODS: Dereplication of ethanol extract by the UPLC-DAD-ESI-MS/MS technique allowed the identification of the major constituents, isolation and identification of alkaloids. The antiplasmodial and cytotoxic activity of the extract, fractions and isolated compounds was evaluated against the chloroquine-resistant W2 strain Plasmodium falciparum and HepG2 cells, respectively...
October 10, 2018: Journal of Pharmacy and Pharmacology
Ji-Ping Li, Ye Yuan, Wen-You Zhang, Zhen Jiang, Tian-Jiao Hu, Yi-Ting Feng, Mo-Xiang Liu
OBJECTIVES: The objective of this paper was to explore the effects of Radix isatidis polysaccharide (RIP) extracted from Radix isatis on alleviating insulin resistance. METHODS: The insulin resistance models of 3T3-L1 preadipocytes and type 2 diabetic rats were established to evaluate the insulin resistance activity of RIP. KEY FINDINGS: Radix isatidis polysaccharide within the concentration range of 25-100 μg/ml could reduce cell supernatant glucose and TNF-α levels (P < 0...
October 9, 2018: Journal of Pharmacy and Pharmacology
Yulei Cui, Lei Jiang, Yun Shao, Lijuan Mei, Yanduo Tao
OBJECTIVES: The hepatoprotective effect of Gentianae macrophyllae root extract (GME) on alcoholic liver disease (ALD) was evaluated through ethanol induced ALD animal model. METHODS: Mice were randomly divided into control normal group (10 mice), ethanol-induced ALD model group (10 mice) and GME plus ethanol group (30 mice). Mice in model group were given intragastric administration with 50% (v/v) ethanol aqueous solution (200 μl for each) once daily for 19 days...
October 9, 2018: Journal of Pharmacy and Pharmacology
Hung Thanh Lam, Bao Le-Vinh, Thi Nhu Quynh Phan, Andreas Bernkop-Schnürch
OBJECTIVES: The aim of this study was to evaluate the cytotoxicity of self-emulsifying drug delivery systems (SEDDS) containing five different cationic surfactants. METHODS: Cationic surfactants were added in a concentration of 1% and 5% (m/m) to SEDDS comprising 30% Capmul MCM, 30% Captex 355, 30% Cremophor EL and 10% propylene glycol. The resulting formulations were characterized in terms of size, zeta potential, in-vitro haemolytic activity and toxicity on Caco-2 via MTT assay and lactate dehydrogenase release assay...
September 25, 2018: Journal of Pharmacy and Pharmacology
Huiying Hua, Julin Yang, Hante Lin, Yang Xi, Manyun Dai, Gangming Xu, Fuyan Wang, Lihong Liu, Tingqi Zhao, Jing Huang, Frank J Gonzalez, Aiming Liu
OBJECTIVES: Metabolic syndrome (MS) is the concurrence of at least three of five medical conditions: obesity, high blood pressure, insulin resistance, high serum triglyceride (TG) and low serum high-density lipoprotein levels. While fibrates are used to treat disorders other than the lowering serum TG, the mechanism by which fibrates decrease MS has not been established. METHODS: In this study, wild-type and Ppara-null mice fed a medium-fat diet (MFD) were administered gemfibrozil and fenofibrate for 3 months respectively, to explore the effect and action mechanism...
September 25, 2018: Journal of Pharmacy and Pharmacology
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