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Journal of Pharmacy and Pharmacology

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https://www.readbyqxmd.com/read/30229910/synthesis-of-new-anticancer-and-anti-inflammatory-isoxazolines-and-aziridines-from-the-natural-deltoin
#1
Mansour Znati, Meriem Debbabi, Anis Romdhane, Hichem Ben Jannet, Jalloul Bouajila
OBJECTIVES: This work describes the synthesis, the bioactivity and the structure-activity relationship of new derivatives from a natural coumarin. METHODS: (-)-Deltoin 1 and the corresponding isoxazolines and aziridines were characterized by spectroscopic means. The cytotoxic (HTC-116, IGROV-1 and OVCAR-3 cancer cell lines) and 5-lipoxygenase activity of (-)-deltoin 1 and its structural analogues have been evaluated. KEY FINDINGS: The phytochemical investigation of the ethyl acetate extract of the flowers of Ferula lutea (Poir...
September 19, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/30203429/the-impact-of-food-intake-on-the-luminal-environment-and-performance-of-oral-drug-products-with-a-view-to-in-vitro-and-in-silico-simulations-a-pearrl-review
#2
REVIEW
Christina Pentafragka, Mira Symillides, Mark McAllister, Jennifer Dressman, Maria Vertzoni, Christos Reppas
OBJECTIVES: Using the type of meal and dosing conditions suggested by regulatory agencies as a basis, this review has two specific objectives: first, to summarize our understanding on the impact of food intake on luminal environment and drug product performance and second, to summarize the usefulness and limitations of available in vitro and in silico methodologies for the evaluation of drug product performance after food intake. KEY FINDINGS: Characterization of the luminal environment and studies evaluating product performance in the lumen, under conditions suggested by regulatory agencies for simulating the fed state, are limited...
September 11, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/30198567/investigation-of-potent-anticarcinogenic-activity-of-1-3-diarylpyrazole-acrylamide-derivatives-in-vitro
#3
Asuman Demiroglu-Zergeroglu, Nurettin Ayvali, Gulseren Turhal, Hurmuz Ceylan, Sultan Nacak Baytas
OBJECTIVES: Pyrazole derivatives are pharmacologically powerful agents pointing at new horizons in the development of anticancer therapies. In this study, anticarcinogenic potential of a series of pyrazole-acrylamide derivatives has been investigated in mesothelial, malignant mesothelioma and lung cancer cell lines. METHODS: The effect of compounds on the viability of cells and the distribution of cell cycle were examined through MTS assay and PI staining, respectively...
September 10, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/30198561/tannins-from-terminalia-chebula-fruits-attenuates-gaba-antagonist-induced-anxiety-like-behaviour-via-modulation-of-neurotransmitters
#4
Yadavalli Chandrasekhar, Garlapati Phani Kumar, Katram Navya, Edavalath Methal Ramya, Kandangath Raghavan Anilakumar
OBJECTIVES: This article investigates the anxiolytic activity of Terminalia chebula tannin-rich extract against picrotoxin (PTX; GABA antagonist)-induced anxiety in mice model. METHODS: Anxiolytic activity was studied by elevated plus maze (EPM), open field test (OFT), light/dark box test (LDT) and Vogel's conflict test (VCT). Electroencephalogram (EEG) was performed to know the changes in brain activity instigated by GABA antagonist. 5-hydroxytryptamine (5-HT), dopamine and norepinephrine levels in brain tissues were estimated by HPLC...
September 10, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/30187488/phytochemistry-and-pharmacology-of-the-genus-entandrophragma-over-the-50-years-from-1967-to-2018-a-golden-overview
#5
REVIEW
Gervais Mouthé Happi, Bonaventure Tchaleu Ngadjui, Ivan Robert Green, Simeon Fogué Kouam
OBJECTIVES: For centuries, the genus Entandrophragma (Meliaceae), endemic to Africa, has been used in traditional medicine for the treatment of several illnesses. This review deals with large range of phytochemicals from the genus Entandrophragma and their pharmacological potentials covering the period from 1967 to 2018. KEY FINDINGS: Phytochemical investigations of the genus Entandrophragma led to the report of about 166 secondary metabolites which have been thoroughly summarized herein including some of their semisynthetic derivatives obtained from chemical transformations as well as their biological activities in the medicinal and agricultural domains...
September 5, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/30187481/bioinformatics-analysis-of-microarray-profiling-identifies-the-mechanism-of-focal-adhesion-kinase-signalling-pathway-in-proliferation-and-apoptosis-of-breast-cancer-cells-modulated-by-green-tea-polyphenol-epigallocatechin-3-gallate
#6
Xiao Luo, Lihua Guo, Lirong Zhang, Yu Hu, Dongmei Shang, Degang Ji
OBJECTIVES: This study aimed to investigate potential gene and signal pathway associated with tumour progression. METHODS: Related microarray data set of breast cancer was obtained from Gene Expression Omnibus database, and differential-expressed genes (DEGs) between two control samples and two treated samples were analysed using statistical software R. We collected 50 epigallocatechin-3-gallate(EGCG)-related genes and 119 breast cancer-related genes to create a knowledge base for following pathway analysis...
September 5, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/30182425/paclitaxel-delivery-system-based-on-poly-lactide-co-glycolide-microparticles-and-chitosan-thermo-sensitive-gel-for-mammary-adenocarcinoma-treatment
#7
Juan I Pesoa, María J Rico, Viviana R Rozados, O Graciela Scharovsky, Julio A Luna, Luciano N Mengatto
OBJECTIVES: To evaluate the combination of more than one release system in the same formulation as a useful strategy to achieve paclitaxel delivery in a more sustained and controlled manner. METHODS: The present study deals with the preparation of poly(lactide-co-glycolide) microparticles loaded with paclitaxel and included in a chitosan thermo-sensitive gelling solution. The microparticles were characterized by their size, shape and drug loading. The formulation was characterized by scanning electron microscopy, in vitro release experiments and was evaluated in mice bearing mammary adenocarcinoma...
September 4, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/30182365/pharmacological-evaluation-of-convolvulus-pluricaulis-as-hypolipidaemic-agent-in-triton-wr-1339-induced-hyperlipidaemia-in-rats
#8
Gaurav Garg, Amol Patil, Jagjit Singh, Nutan Kaushik, Ajay Praksah, Arnab Pal, Amitava Chakrabarti
OBJECTIVE: The aim of the study was to evaluate the effect of Convolvulus pluricaulis (CP; C. pluricaulis) methanolic extract on Triton WR-1339-induced hyperlipidaemia in rats. METHODS: The study comprised of six groups namely normal control, experimental control and treatment groups (100, 200 and 400 mg/kg of C. pluricaulis, and 65 mg/kg of Fenofibrate). Hyperlipidaemia was induced by a single intraperitoneal injection of Triton WR-1339 400 mg/kg in rats. Parameters such as lipid profile, oxidative stress, histological analysis and atherogenic index were evaluated...
September 4, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/30175489/dimethyl-fumarate-interferes-with-myd88-dependent-toll-like-receptor-signalling-pathway-in-isoproterenol-induced-cardiac-hypertrophy-model
#9
Asmaa A Ahmed, Amany A E Ahmed, Engy M El Morsy, Shahira Nofal
OBJECTIVES: To investigate the effect of dimethyl fumarate (DMF) on Toll-like receptor (TLR) signalling pathway in isoproterenol (ISO)-induced cardiac hypertrophy in rats. METHODS: Sixty adult male Sprague-Dawley rats were randomly allocated into three groups. group I: rats received the vehicles only; group II: rats were treated with ISO (5 mg/kg per day S.C.) to induce cardiac hypertrophy for 7 days; and group III: rats were given DMF (25 mg/kg per 12 h P.O.) for 28 days, and at the last 7 days, they were treated with ISO (5 mg/kg per day S...
September 2, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/30168133/preparation-characterization-and-antimicrobial-activity-of-inclusion-complex-of-biochanin-a-with-2-hydroxypropyl-%C3%AE-cyclodextrin
#10
Ivana Lj Nikolic, Ivan M Savic, Mirjana M Popsavin, Srdjan J Rakic, Tatjana M Mihajilov-Krstev, Ivan S Ristic, Suzana P Eric, Ivana M Savić-Gajic
OBJECTIVES: An inclusion complex of biochanin A (BCA) with (2-hydroxypropyl)-β-cyclodextrin (HP-β-CD) was prepared in the ethanol solution to improve its water solubility. METHODS: Using the FTIR, 1 H-NMR, XRD, DSC and SEM methods, the structural characterization of the prepared complex was analysed. KEY FINDINGS: The phase-solubility study has shown that the solubility of BCA was increased twofold in 42% (v/v) ethanol solution after complexation with HP-β-CD...
August 31, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/30168142/virucidal-antiviral-and-immunomodulatory-activities-of-%C3%AE-escin-and-aesculus-hippocastanum-extract
#11
Flavia M Michelini, Laura E Alché, Carlos A Bueno
OBJECTIVES: β-Escin, one of the constituents of Aesculus hippocastanum L. (Hippocastanaceae) seed extract (AH), inhibits NF-κB activation, which plays an important role in HSV-1 replication. The aim was to examine the antiherpetic activity of β-escin and AH, as well as their effect on the activation of NF-κB and AP-1 and cytokine secretion in epithelial cells and macrophages. METHODS: Cell viability was evaluated using MTT assay, and antiviral and virucidal activity was determined by plaque assay...
August 30, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/30159909/assessment-of-the-cytotoxic-potential-of-an-aqueous-ethanolic-extract-from-thalassia-testudinum-angiosperm-marine-grown-in-the-caribbean-sea
#12
Idania Rodeiro, Ivones Hernández, José A Herrera, Mario Riera, Maria T Donato, Laia Tolosa, Kethia González, Yadira Ansoar, Maria J Gómez-Lechón, Wim Vanden Berghe, Miriam Lopes
OBJECTIVES: Reported antioxidant, anti-inflammatory and neuroprotective properties for one aqueous-ethanolic extract from Thalassia testudinum which grows in the Caribbean Sea compelled us to explore about extract cytotoxic effects. METHODS: Cell viability was assayed on tumour (HepG2, PC12, Caco-2 and 4T1) and non-tumour (VERO, 3T3, CHO, MCDK and BHK2) cell lines. The extract effects upon primary cultures of rat and human hepatocytes and human lymphocytes were assayed...
August 30, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/30159900/mir-324-5p-reduces-viability-and-induces-apoptosis-in-gastric-cancer-cells-through-modulating-tspan8
#13
Hai Lin, Ai-Jun Zhou, Jing-Yu Zhang, Shu-Fang Liu, Jian-Xiang Gu
OBJECTIVES: The purpose of this study was to further clarify the role and underlying mechanism of miR-324-5p in gastric cancer. METHODS: The expressions of miR-324-5p and TSPAN8 as determined by qRT-PCR or Western blot were compared between the gastric cancer tissues and normal tissues. Human gastric cancer cell line SGC-7901 was cultured and transfected with miR-324-5p mimic/inhibitor or pcDNA-TSPAN8. The cell survival was assessed by the cell viability and apoptosis...
August 29, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/30141195/anticancer-properties-of-lipid-and-poly-%C3%AE%C2%B5-caprolactone-nanocapsules-loaded-with-ferrocenyl-tamoxifen-derivatives
#14
Feten Najlaoui, Pascal Pigeon, Sonia Aroui, Mylène Pezet, Lucie Sancey, Naziha Marrakchi, Ali Rhouma, Gérard Jaouen, Michel De Waard, Benoit Busser, Stéphane Gibaud
OBJECTIVE: We synthesized new tamoxifen derivatives as anticancer drug candidates and elaborated on convection-enhanced delivery (CED) as a strategy for delivery. METHODS: To overcome the issue of their poor solubility, these ferrocenyl-tamoxifen derivatives were esterified and encapsulated into different nanocarriers, that is lipid (LNC) and polymeric nanocapsules (PNL-NC). We describe the chemistry, the encapsulation and the physicochemical characterization of these formulations...
August 23, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/30136729/antifungal-and-cytotoxicity-activities-of-banisteriopsis-argyrophylla-leaves
#15
Daiane M Oliveira, Tomás F R Silva, Mário M Martins, Sérgio A L de Morais, Roberto Chang, Francisco J T de Aquino, Claudio V da Silva, Thaise L Teixeira, Carlos H G Martins, Thaís S Moraes, Luís C S Cunha, Marcos Pivatto, Alberto de Oliveira
OBJECTIVES: This work aimed to evaluate the antifungal and cytotoxic activity of the EtOH extract and fractions of Banisteriopsis argyrophylla leaves, and to perform the identification of these bioactive metabolites. METHODS: The EtOAc fraction (EAF) obtained from the ethanolic extract of B. argyrophylla leaves showed better antifungal potential against Candida spp. In this fraction, ten flavonoids have been identified by UHPLC-ESI-MSn . Then, EAF was submitted to column chromatography to give four new fractions (A1-A4)...
August 23, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/30132896/topical-emulsion-containing-pyrrolidine-dithiocarbamate-effectiveness-against-ultraviolet-b-irradiation-induced-injury-of-hairless-mouse-skin
#16
Renata M Martinez, Ana L M Ivan, David L Vale, Marcela Z Campanini, Vitor S Ferreira, Vinicius S Steffen, Fabiana T M C Vicentini, Fernanda M P Vilela, Maria J V Fonseca, Marcela M Baracat, Sandra R Georgetti, Waldiceu A Verri, Rúbia Casagrande
OBJECTIVES: To evaluate the effects of a topical emulsion containing pyrrolidine dithiocarbamate (PDTC) (EcPDTC) in skin oxidative stress and inflammation triggered by ultraviolet B (UVB) irradiation (dose of 4.14 J/cm2 ). METHODS: Hairless mouse received treatment with 0.5 g of EcPDTC or control emulsion (CTRLE) on the dorsal surface skin 12 h, 6 h and 5 min before and 6 h after the irradiation. Oxidative stress was evaluated by ferric reducing antioxidant power (FRAP), 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) radical (ABTS) scavenging capacity, reduced glutathione quantitation, catalase activity, superoxide anion production and lipid peroxidation products...
August 22, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/30079513/multiclass-mycotoxins-in-lotus-seeds-analysed-by-an-isotope-labelled-internal-standard-based-uplc-ms-ms
#17
Pinxuan Huang, Weijun Kong, Sha Wang, Ruilin Wang, Jinghua Lu, Meihua Yang
OBJECTIVES: This study aimed to explore the residue levels of multiclass mycotoxins in medicinal and edible lotus seeds. METHODS: A rapid and reliable isotope-labelled internal standard-based UPLC-MS/MS method was developed and validated for sensitive and accurate analysis of multiclass mycotoxins including aflatoxins (AFB1 , AFB2 , AFG1 and AFG2 ), ochratoxin A (OTA), zearalenone (ZEN), deoxynivalenol (DON), fumonisins (FB1 and FB2 ), T-2 and HT-2 toxins in lotus seeds...
August 5, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/30073654/comparative-evaluation-of-four-triterpenoid-glycoside-saponins-of-bacoside-a-in-alleviating-sub-cellular-oxidative-stress-of-n2a-neuroblastoma-cells
#18
Pragya Bhardwaj, Chakresh Kumar Jain, Ashwani Mathur
OBJECTIVES: To examine the neuroprotective property of triterpenoid glycoside saponins of Bacopa monnieri (L.) Wettst. bacoside A and its components against H2 O2 -induced oxidative stress on neuronal (N2a) cells. METHODS: The cytoprotective effects of individual bacoside A components were evaluated towards oxidative stressed neuronal cells. Bacoside A was screened for neuronal cell viability (MTT assay) and change in intracellular reactive oxygen species (ROS), anti-apoptotic properties and mitochondrial membrane potential (MMP) using fluorescence microscopy...
August 2, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/30070363/lipophilicity-and-hydrophobicity-considerations-in-bio-enabling-oral-formulations-approaches-a-pearrl-review
#19
REVIEW
Felix Ditzinger, Daniel J Price, Alexandra-Roxana Ilie, Niklas J Köhl, Sandra Jankovic, Georgia Tsakiridou, Simone Aleandri, Lida Kalantzi, René Holm, Anita Nair, Christoph Saal, Brendan Griffin, Martin Kuentz
OBJECTIVES: This review highlights aspects of drug hydrophobicity and lipophilicity as determinants of different oral formulation approaches with specific focus on enabling formulation technologies. An overview is provided on appropriate formulation selection by focussing on the physicochemical properties of the drug. KEY FINDINGS: Crystal lattice energy and the octanol-water partitioning behaviour of a poorly soluble drug are conventionally viewed as characteristics of hydrophobicity and lipophilicity, which matter particularly for any dissolution process during manufacturing and regarding drug release in the gastrointestinal tract...
August 2, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/30062750/effects-of-medicines-used-to-treat-gastrointestinal-diseases-on-the-pharmacokinetics-of-coadministered-drugs-a-pearrl-review
#20
REVIEW
Chara Litou, Angela Effinger, Edmund S Kostewicz, Karl J Box, Nikoletta Fotaki, Jennifer B Dressman
OBJECTIVES: Drugs used to treat gastrointestinal diseases (GI drugs) are widely used either as prescription or over-the-counter (OTC) medications and belong to both the 10 most prescribed and 10 most sold OTC medications worldwide. The objective of this review article is to discuss the most frequent interactions between GI and other drugs, including identification of the mechanisms behind these interactions, where possible. KEY FINDINGS: Current clinical practice shows that in many cases, these drugs are administered concomitantly with other drug products...
July 30, 2018: Journal of Pharmacy and Pharmacology
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