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Journal of Pharmacy and Pharmacology

Jinfang Zhu, Mengying Hu, Liyan Qiu
OBJECTIVES: This study aimed to evaluate that the polymersomes (Ps-DOX-CA4P) dual-loaded with combretastatin-A4 phosphate (CA4P) and doxorubicin (DOX) overcame drug resistance and sensitized tumour cells to chemotherapeutic drugs. METHODS: Ps-DOX-CA4P were prepared by solvent evaporation method using mPEG-b-PLA as carriers. The potential capability of CA4P to reverse DOX resistance was verified by cytotoxicity test, apoptosis assay and cellular uptake of DOX. The comparison between free drugs and drug-loaded polymersomes was also made on a single-layer cell model and multicellular tumour spheroids to display the superiority of the drug vehicles...
April 20, 2017: Journal of Pharmacy and Pharmacology
Alam Zeb, Omer S Qureshi, Hoo-Seong Kim, Myung-Sic Kim, Jong-Ho Kang, Jeong-Sook Park, Jin-Ki Kim
OBJECTIVES: The aim of this study was to develop high payload itraconazole-incorporated lipid nanoparticles (HINP) with modulated release property using a binary mixture core of solid and liquid lipid for oral and parenteral administration. METHODS: High payload itraconazole-incorporated lipid nanoparticles were prepared by hot high-pressure homogenization method using tristearin (TS) as a solid lipid, triolein (TO) as a liquid lipid and egg phosphatidylcholine/Tween 80/DSPE-PEG2000 as a surfactants mixture...
April 18, 2017: Journal of Pharmacy and Pharmacology
Priyanka Kriplani, Kumar Guarve, Uttam S Baghael
OBJECTIVES: Arnica montana is a widely used therapeutic plant used traditionally to treat various ailments. The objective of this study was to evaluate the botany, phytochemistry and ethnopharmacology along with special emphasis given on pharmacological activity of plant A. montana. KEY FINDINGS: The plant extracts have been reported to possess antibacterial, antitumor, antioxidant, anti-inflammatory, antifungal and immunomodulatory activity. A wide range of chemical compounds including sesquiterpene lactones and their short-chain carbonic acid esters, flavonoids, carotenoids, essential oils, diterpenes, arnidiol, pyrrolizidine alkaloids, coumarins, phenolic acids, lignans and oligosaccharides, etc...
April 11, 2017: Journal of Pharmacy and Pharmacology
Tatiana V Bomko, Tatiana N Nosalskaya, Tatiana V Kabluchko, Yury V Lisnyak, Artur V Martynov
OBJECTIVES: Currently, probiotics are increasingly used as the alternative to antibiotics as well as the preventive measures in humans. In particular, probiotics occupy a key position in the treatment of antibiotics-associated intestinal dysbiosis. A spore-forming microorganism lactobacillus Bacillus coagulans is one of the most promising probiotics. However, some of its pharmacological effects remain poorly understood. This study was aimed at investigation of the effect of B. coagulans (Laktovit Forte) on the intestinal dysbiosis syndrome in mice caused by streptomycin against the background of cyclophosphamide-induced cellular immunodeficiency...
April 11, 2017: Journal of Pharmacy and Pharmacology
Tapan K Dash, Venkata Sai Badireenath Konkimalla
OBJECTIVE: The prime objective of current work was to develop a strategy for preparation of combinational nano-formulation for reversal of drug resistance. METHODS: As a model system, doxorubicin (DOX)-resistant COLO205 cells were developed and validated. From co-treatment studies with DOX, curcumin was selected as it reversed DOX-resistance at lowest concentration. In an attempt to increase its solubility, curcumin was encapsulated into hydroxypropyl-β-cyclodextrin (HP-β-CD)...
April 11, 2017: Journal of Pharmacy and Pharmacology
Dahae Lee, Ki Hyun Kim, Jaemin Lee, Gwi Seo Hwang, Hye Lim Lee, Dae-Hyun Hahm, Chang Ki Huh, Sang Cheon Lee, Sanghyun Lee, Ki Sung Kang
OBJECTIVES: Maintaining glucose homoeostasis is essential for the survival of cells. Despite the various health benefits of Korean thistle (Cirsium japonicum var. maackii), their effects on pancreatic β-cell apoptosis in type 1 diabetes mellitus and the underlying mechanisms remain unclear, and experimentally investigated in this study. METHODS: The effects of C. japonicum var. maackii and its active component cirsimaritin against streptozotocin (STZ)-induced cytotoxicity were assessed in INS-1 cells...
April 11, 2017: Journal of Pharmacy and Pharmacology
Jan Schmidt, Polonca Ferk
OBJECTIVES: Much research has been performed on the field of identifying the roles of adenosine and adenosinergic signalling, but a relatively low number of marketing authorizations have been granted for adenosine receptor (AdR) ligands. In part, this could be related to their safety issues; therefore, our aim was to examine the toxicological and adverse effects data of different compounds acting on adenosinergic signalling, including different AdR ligands and compounds resembling the structure of adenosine...
April 11, 2017: Journal of Pharmacy and Pharmacology
Nittaya Jiamvoraphong, Nattinee Jantaratnotai, Pantip Sanvarinda, Patoomratana Tuchinda, Pawinee Piyachaturawat, Anusorn Thampithak, Pimtip Sanvarinda
OBJECTIVE: We investigated the molecular mechanisms underlying the effect of (3S)-1-(3,4-dihydroxyphenyl)-7-phenyl-(6E)-6-hepten-3-ol, also known as compound 092, isolated from Curcuma comosa Roxb on the production of pro-inflammatory mediators and oxidative stress in lipopolysaccharide (LPS)-activated highly aggressive proliferating immortalized (HAPI) microglial cell lines. METHOD: Nitric oxide (NO) production was determined using the Griess reaction, and reverse transcription polymerase chain reaction was used to measure the expression of inducible nitric oxide synthase (iNOS) mRNA...
April 6, 2017: Journal of Pharmacy and Pharmacology
Vianey de la Rosa-Lugo, Macdiel Acevedo-Quiroz, Myrna Déciga-Campos, María Yolanda Rios
OBJECTIVE: To establish the role of TRPV1 receptor in the antinociceptive effect of natural alkamides (i.e. affinin, longipinamide A, longipenamide A and longipenamide B) isolated from Heliopsis longipes (A. Gray) S.F. Blake and some related synthetic alkamides (i.e. N-isobutyl-feruloylamide and N-isobutyl-dihydroferuloylamide). METHODS: The orofacial formalin test was used to assess the antinociceptive activity of natural (1-30 μg, orofacial region) and synthetic alkamides (0...
April 4, 2017: Journal of Pharmacy and Pharmacology
Trevor A Stump, Brittany N Santee, Lauren P Williams, Rachel A Kunze, Chelsae E Heinze, Eric D Huseman, Rebecca J Gryka, Denise S Simpson, Samson Amos
OBJECTIVES: Glioblastoma (GBM) is highly proliferative, infiltrative, malignant and the most deadly form of brain tumour. The epidermal growth factor receptor (EGFR) is overexpressed, amplified and mutated in GBM and has been shown to play key and important roles in the proliferation, growth and survival of this tumour. The goal of our study was to investigate the antiproliferative, apoptotic and molecular effects of apigenin in GBM. METHODS: Proliferation and viability tests were carried out using the trypan blue exclusion, MTT and lactate dehydrogenase (LDH) assays...
March 28, 2017: Journal of Pharmacy and Pharmacology
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
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
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
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
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
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
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
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
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
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
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