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Journal of Pharmacy and Pharmacology

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https://www.readbyqxmd.com/read/29774523/acute-and-subacute-antidiabetic-studies-of-enp-9-a-new-1-5-diarylpyrazole-derivative
#1
Eduardo Hernández-Vázquez, Sandra Young-Peralta, Litzia Cerón-Romero, Sara García-Jiménez, Samuel Estrada-Soto
OBJECTIVES: To explore the antihyperglycaemic and antidiabetic effects and to determine the acute toxicity of 5-(4-chlorophenyl)-1-(2,4-dichloro-phenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide (ENP-9). METHODS: The antihyperglycaemic effect of ENP-9 (50 mg/kg) was determined by oral glucose tolerance test (OGTT). Also, the acute (16, 50 and 160 mg/kg) and subacute (50 mg/kg/day for 10 days) antidiabetic effects of ENP-9 were determined. After subacute treatment, blood samples were analysed to determine glucose and lipid profiles...
May 17, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29770446/anticancer-activity-of-tetrandrine-by-inducing-pro-death-apoptosis-and-autophagy-in-human-gastric-cancer-cells
#2
Xin-Yu Bai, Yuan-Gui Liu, Wu Song, Ying-Ying Li, Dong-Shun Hou, Hao-Ming Luo, Ping Liu
OBJECTIVES: To investigate the antitumour property of tetrandrine by inducing autophagy and apoptosis in human gastric cancer cells, and to explore the potential molecular mechanisms. METHODS: The antitumour activity of tetrandrine was assessed through MTT assay. Apoptosis was measured by flow cytometry and microscopic examination of cellular morphology. The mitochondrial membrane potential was detected by staining with Rh-123. Induction of autophagy was monitored by transmission electron microscopy observation, using GFP-LC3 transfection...
May 16, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29770444/pueraria-tuberosa-extract-inhibits-inos-and-il-6-through-suppression-of-pkc-%C3%AE-and-nf-kb-pathway-in-diabetes-induced-nephropathy
#3
Rashmi Shukla, Somanshu Banerjee, Yamini B Tripathi
OBJECTIVES: Inflammation plays an important role in the pathogenesis of diabetic nephropathy (DN). The aim of this study was to explore the anti-inflammatory role of PTY-2r (extracted from Pueraria tuberosa), on streptozotocin (STZ)-induced DN rats. METHODS: Diabetes was induced by intraperitoneal injection of STZ (55mg/kg) in rats. After 60 days, the rats were randomly divided into three groups (n = 6/each group), namely DN control group 2, DN rats treated with PTY-2r at dose of 100 mg/100 g, group 3 and 50 mg/100 g, group 4, p...
May 16, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29770441/evaluation-of-the-anti-inflammatory-activity-of-tinospora-cordifolia-willd-miers-chloroform-extract-a-preclinical-study
#4
Sheena Philip, Greeshma Tom, Asha V Vasumathi
OBJECTIVES: Tinospora cordifolia (Willd.) Miers is an inevitable ingredient of Ayurvedic rasayanas for the treatment of disorders with unregulated inflammation. However, studies regarding the mechanism of anti-inflammatory potential of this plant at the molecular level are lacking. METHODS: In vitro evaluations were conducted in RAW264.7 macrophages which were preincubated with chloroform extract of T. cordifolia (CETC) and subsequently stimulated with LPS. The expressions of COX-2, TNF-α and iNOS genes were analysed by SQRT-PCR and Western blot, cytokines (IL-6, IL-1β and PGE2 ) levels by ELISA, NF-κB activation and p38 MAPK phosphorylation by Immunoblot and confocal imaging...
May 16, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29770440/approaches-to-increase-mechanistic-understanding-and-aid-in-the-selection-of-precipitation-inhibitors-for-supersaturating-formulations-a-pearrl-review
#5
REVIEW
Daniel J Price, Felix Ditzinger, Niklas J Koehl, Sandra Jankovic, Georgia Tsakiridou, Anita Nair, René Holm, Martin Kuentz, Jennifer B Dressman, Christoph Saal
OBJECTIVES: Supersaturating formulations hold great promise for delivery of poorly soluble active pharmaceutical ingredients (APIs). To profit from supersaturating formulations, precipitation is hindered with precipitation inhibitors (PIs), maintaining drug concentrations for as long as possible. This review provides a brief overview of supersaturation and precipitation, focusing on precipitation inhibition. Trial-and-error PI selection will be examined alongside established PI screening techniques...
May 16, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29766510/ineffectiveness-of-saxagliptin-as-a-neuroprotective-drug-in-6-ohda-lesioned-rats
#6
Joelle de Melo Turnes, Taysa Bervian Bassani, Leonardo C Souza, Maria A B F Vital
OBJECTIVES: To determine whether the drug saxagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor which is utilized for the treatment of Diabetes Mellitus, has neuroprotective effects in the animal model of Parkinson's disease (PD) induced by 6-hydroxydopamine (6-OHDA) in rats. METHODS: Male Wistar rats (weighing 280-300 g) received a bilateral infusion of 6-OHDA in the substantia nigra. Twenty-four hours later, they were treated with saxagliptin (1 mg/kg, p.o) once daily, for 21 days...
May 16, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29766501/impact-of-gastrointestinal-disease-states-on-oral-drug-absorption-implications-for-formulation-design-a-pearrl-review
#7
REVIEW
Angela Effinger, Caitriona M O'Driscoll, Mark McAllister, Nikoletta Fotaki
OBJECTIVES: Drug product performance in patients with gastrointestinal (GI) diseases can be altered compared to healthy subjects due to pathophysiological changes. In this review, relevant differences in patients with inflammatory bowel diseases, coeliac disease, irritable bowel syndrome and short bowel syndrome are discussed and possible in vitro and in silico tools to predict drug product performance in this patient population are assessed. KEY FINDINGS: Drug product performance was altered in patients with GI diseases compared to healthy subjects, as assessed in a limited number of studies for some drugs...
May 16, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29761870/intestinal-disposition-of-quercetin-and-its-phase-ii-metabolites-after-oral-administration-in-healthy-volunteers
#8
Clément Chalet, Jari Rubbens, Jan Tack, Guus S Duchateau, Patrick Augustijns
OBJECTIVES: Quercetin is one of the main dietary flavonoids and undergoes a substantial intestinal phase-II metabolism. Quercetin conjugates have been detected in plasma and in urine, but their presence in the small intestine has not been assessed. This study aimed to investigate the intestinal metabolism and metabolite excretion of quercetin by the human small intestinal wall after oral dosing. METHODS: Six healthy volunteers were given a capsule of 500 mg of quercetin with 240 ml of water...
May 15, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29761837/augmentation-of-the-cytotoxic-effects-of-nitrogen-containing-bisphosphonates-in-hypoxia
#9
Tetsuya Minegaki, Saya Koiki, Yutaro Douke, Chihiro Yamane, Ai Suzuki, Misato Mori, Masayuki Tsujimoto, Kohshi Nishiguchi
OBJECTIVES: Tumour hypoxia is a major obstacle in cancer therapy that leads to poor prognosis. Therefore, the development of cancer treatments that are effective in hypoxia is necessary. Nitrogen-containing bisphosphonates (N-BPs), which are used to treat bone disease, are cytotoxic to several cancer cells in normoxia. Therefore, we investigated the cytotoxicity of N-BPs in cancer cells in hypoxia. METHODS: We studied the cytotoxicities of N-BPs, statins and anticancer drugs in human cancer cells under hypoxic conditions (1% O2 )...
May 15, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29744882/evaluation-of-cytotoxic-immunomodulatory-and-antibacterial-activities-of-aqueous-extract-from-leaves-of-conocarpus-erectus-linnaeus-combretaceae
#10
Dayane Kelly Dias do Nascimento Santos, Vanessa Silva de Almeida, Daniel Rodrigo Cavalcante de Araujo, Wolfgang Harand, Ana Karine de Araújo Soares, Leyllane Rafael Moreira, Virgínia Maria Barros de Lorena, Lucimeri Paulino Machado Magalhães, Rafael Matos Ximenes, Kêsia Xisto da Fonseca Ribeiro de Sena, Cristiane Moutinho Lagos de Melo, Thiago Henrique Napoleão, Cláudia Sampaio de Andrade Lima, Ricardo Yara, Jeymesson Raphael Cardoso Vieira
OBJECTIVES: This work evaluated the antibacterial activity, cytotoxicity and immunomodulatory effect on human peripheral blood mononuclear cells (PBMCs) promoted by aqueous extract from Conocarpus erectus leaves (AELCe). METHODS: The extract was characterized by thin layer chromatography and ultraperformance liquid chromatography coupled to mass spectrometry (UPLC-MS). Cytotoxicity of AELCe (6.25-50 μg/ml) was investigated using annexin V and propidium iodide. Cytokine and nitric oxide levels in PBMCs culture supernatants exposed or not to AELCe (12...
May 10, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29726011/mir-505-mediates-methotrexate-resistance-in-colorectal-cancer-by-targeting-rassf8
#11
Yalin Chen, Li Bian, Yingmei Zhang
OBJECTIVE: To investigate the relationship between miR-505 and RASSF8 as well as the effect of miR-505 on methotrexate (MTX) resistance of human colorectal cancer (CRC). METHODS: Microarray was used to select differentially expressed miRNAs. QRT-PCR and western blot were performed to assess miR-505 and RASSF8 mRNA levels in MTX-sensitive and MTX-resistant CRC tissues and cells. Cell viability, propagation and apoptosis were confirmed by MTT, colony formation assays and flow cytometry...
May 3, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29708588/anti-arthritic-properties-of-crude-extract-from-chenopodium-ambrosioides-l-leaves
#12
Wanderson S Pereira, Girlaine P da Silva, Mariana V Vigliano, Nathalia R F Leal, Fabiana A Pinto, Daniele C Fernandes, Shirley V M Santos, Thiago Martino, Johnny R Nascimento, Ana Paula S de Azevedo, Eduardo N Fonseca, Leosvaldo S M Velozo, Lauro R Souza Neto, Frederico F Bastos, Elyzabeth A Portari, Kátia C Carvalho Sabino, Flávia Nascimento, Marsen G P Coelho
OBJECTIVES: To evaluate the effect of hydroalcoholic crude extract (HCE) from Chenopodium ambrosioides leaves on the development of type II collagen-induced arthritis (CIA) and on pro-inflammatory cytokine balance. METHODS: Collagen-induced arthritis was induced in DBA1/J mice. On the 21st day, the mice were treated orally with HCE or methotrexate, daily. Six weeks after beginning the treatment, the following measures were determined: lymphoid organs cell numbers, percentage of blood cells, IL-6, IFN-γ, TNF-α and IL-17 serum concentrations, activity of hepatic and kidney glutathione S-transferase, hepatic 7-ethoxyresorufin-O-deethylase activity, bone density and histopathology...
April 30, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29682750/the-effect-of-phloretin-on-synaptic-proteins-and-adult-hippocampal-neurogenesis-in-a%C3%AE-1-42-injected-male-wistar-rats
#13
Priya Ghumatkar, Vaibhavi Peshattiwar, Sachin Patil, Suraj Muke, David Whitfield, David Howlett, Paul Francis, Sadhana Sathaye
OBJECTIVES: Considering the deleterious effect of Aβ1-42, a study was designed to evaluate the effect of phloretin on altered synaptic proteins and adult hippocampal neurogenesis in Aβ1-42-injected Wistar rats. METHODS: The rats were pretreated with 5 mg/kg p.o dose of phloretin and donepezil (positive control) for 28 days, followed by intrahippocampal injections of aggregated Aβ1-42. After termination, perfused brains were isolated and subjected to Western blot and immunohistochemistry (IHC) analysis...
April 23, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29675844/delivery-of-therapeutics-for-deep-seated-ocular-conditions-status-quo
#14
REVIEW
Hubert Nguyen, Shawn Eng, Thanh Ngo, Crispin R Dass
OBJECTIVES: There is a need for research into designing effective pharmaceutical systems for delivering therapeutic drugs to the posterior of the eye for glaucoma-related pathology, macular degeneration, diabetic retinopathy, macular oedema, retinitis and choroiditis. Conventionally, eye drops have been extensively utilised for topical drug delivery to the anterior segment of the eye, but are less effective for delivery of therapeutics to the back of the eye due to significant barriers hampering drug penetration into the target intraocular tissue...
April 19, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29663387/muscarinic-and-nicotinic-acetylcholine-receptor-agonists-current-scenario-in-alzheimer-s-disease-therapy
#15
REVIEW
Stuti Verma, Ashwini Kumar, Timir Tripathi, Awanish Kumar
OBJECTIVES: Alzheimer's disease (AD) has become the primary cause of dementia. It shows a progressive cognitive dysfunction with degenerating neurons. Acetylcholine receptors (AChRs) propagate the cognitive ability and it consists of two primary members namely muscarinic (mAChRs) and nicotinic receptors (nAChRs). Where mAChRs is G-protein coupled receptor, (nAChRs) are ligand-gated ion channels. The conventional therapeutic regimen for AD consists of three acetylcholinestearse inhibitors while a single NMDA receptor antagonist...
April 16, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29635685/the-pig-as-a-preclinical-model-for-predicting-oral-bioavailability-and-in-vivo-performance-of-pharmaceutical-oral-dosage-forms-a-pearrl-review
#16
REVIEW
Laura J Henze, Niklas J Koehl, Joseph P O'Shea, Edmund S Kostewicz, René Holm, Brendan T Griffin
OBJECTIVES: In pharmaceutical drug development, preclinical tests in animal models are essential to demonstrate whether the new drug is orally bioavailable and to gain a first insight into in vivo pharmacokinetic parameters that can subsequently be used to predict human values. Despite significant advances in the development of bio-predictive in vitro models and increasing ethical expectations for reducing the number of animals used for research purposes, there is still a need for appropriately selected pre-clinical in vivo testing to provide guidance on the decision to progress to testing in humans...
April 10, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29635682/hydroxypropyl-%C3%AE-cyclodextrin-containing-hydrogel-enhances-skin-formononetin-permeation-retention
#17
Paula Hollweg Dias, Marina Scopel, Simony Martiny, Sara Elis Bianchi, Valquiria Linck Bassani, José Angelo Silveira Zuanazzi
OBJECTIVES: This study was aimed to investigate the in vitro permeation potential of hydrogel formulations containing the isoflavones formononetin and biochanin A and cyclodextrins in different combinations. METHODS: The permeation assay was performed using porcine skin discs on Franz diffusion cells model. The isoflavone contents of the formulations were quantified in the different layers of the skin using a validated HPLC-PDA method. KEY FINDINGS: The isoflavones individually incorporated into the formulations showed high permeation potential, especially formononetin, after the incorporation of hydroxypropyl-β-cyclodextrin that enhanced its permeation in the epidermis and dermis...
April 10, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29633270/is-the-demonstration-of-bioequivalence-for-clavulanic-acid-required-in-amoxicillin-clavulanic-acid-orally-administered-immediate-release-products
#18
Naseem A Charoo, Ziyaur Rahman, Areeg Anwer Ali
OBJECTIVES: Bioequivalence (BE) criteria for amoxicillin-clavulanic acid (Co-amoxiclav) oral formulations are based on 90% confidence interval for both amoxicillin and clavulanic acid. The aim of this work is to explore the relevance of demonstrating BE of clavulanic acid in Co-amoxiclav oral formulations and also to assess the impact on safety and efficacy of product due to bioinequivalent clavulanic acid. METHODS AND KEY FINDINGS: The subtherapeutic levels of clavulanic acid would continue to exert their action against β-lactamases due to postβ-lactamase inhibitor effect...
April 6, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29633269/effects-of-lidocaine-and-the-inclusion-complex-with-2-hydroxypropyl-%C3%AE-cyclodextrin-on-cell-viability-and-proliferation-of-oral-squamous-cell-carcinoma
#19
Luiz E N Ferreira, Gabriela B M Antunes, Bruno V Muniz, Jonny Burga-Sánchez, Nathalie F S de Melo, Francisco C Groppo, Leonardo F Fraceto, Maria C Volpato
OBJECTIVES: Squamous cell carcinoma (SCC) is a malignant disease that affects the oral cavity. Lidocaine has shown antiproliferative and cytotoxic activity on several cell types. The rapid dispersion is a limitation issue; however, the complexation in cyclodextrin improved pharmacological features and modified the drug release. This study investigated the effects of lidocaine (lido) complexed with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD-lido) on cell viability and proliferation of human tongue squamous cell carcinoma SCC9 and SCC25...
April 6, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29633259/antimutagenic-constituents-from-monanthotaxis-caffra-sond-verdc
#20
Rhulani Makhuvele, Kenn Foubert, Sandra Apers, Luc Pieters, Luc Verschaeve, Esameldin Elgorashi
OBJECTIVES: Monanthotaxis caffra (Sond.) Verdc. (Annonaceae) has been reported to possess antitumoural properties. Preliminary screening showed that the crude methanolic leaf extract had strong antimutagenic effects against aflatoxin B1 -induced mutagenicity. The aim of this study was to isolate and evaluate the antimutagenic properties of the active constituents from M. caffra. METHODS: Different chromatographic, spectroscopic and spectrometric techniques were used for the isolation and identification of the antimutagenic constituents...
April 6, 2018: Journal of Pharmacy and Pharmacology
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