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Journal of Pharmacy and Pharmacology

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https://www.readbyqxmd.com/read/28543298/synthesis-and-preclinical-pharmacokinetic-study-of-dha-10-a-novel-potential-antifungal-pogostone-analogue
#1
Ming Liu, Yanfen Zhou, Jianwei Zhu, Bo Ma, Zheng Fang, Qi Zhang
OBJECTIVES: The emergence of fungal disease calls for the urgency of development of novel drug. In this study, we developed a novel pogostone analogue, DHA-10 and investigated its preclinical pharmacokinetics, tissue distribution, excretion and protein binding rate in rats. METHODS: DHA-10 was synthesized with dehydroacetic acid (DHA) as the starting material and the structure confirmed by NMR and HRMS. The LC-MS/MS was applied to quantitative analysis of DHA-10 concentrations in the biological samples...
May 23, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28543088/3d-quantitative-structure-activity-relationship-and-docking-studies-of-coumarin-derivatives-as-tissue-kallikrein-7-inhibitors
#2
Xin Zheng, Mengxi He, Xiao Tan, Jun Zheng, Fangyu Wang, Sen Liu
OBJECTIVES: Kallikrein 7 (KLK7) is a secreted serine protease that plays important roles in skin desquamation and tumour progression, which makes it an attracting drug target. To guide the design of KLK7 inhibitors, a series of coumarin-based inhibitors were used to perform 3D-quantitative structure-activity relationship analysis. METHODS: 3D conformations of 37 inhibitors were generated and used to construct CoMFA and CoMSIA models. Then a complex model between the inhibitors and KLK7 was built with molecular docking...
May 23, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28543032/influence-of-different-wild-garlic-allium-ursinum-extracts-on-the-gastrointestinal-system-spasmolytic-antimicrobial-and-antioxidant-properties
#3
Dragana R Pavlović, Milica Veljković, Nikola M Stojanović, Marija Gočmanac-Ignjatović, Tatjana Mihailov-Krstev, Suzana Branković, Dušan Sokolović, Mirjana Marčetić, Niko Radulović, Mirjana Radenković
OBJECTIVES: As there are no previous studies of the European wild-garlic (Allium ursinum) effects on the gastrointestinal system, despite its traditional applications in gastrointestinal disorders' treatment and regular use in the human diet, we have quantified and compared spasmolytic, antimicrobial and antioxidant activities of its different leaf extracts. METHODS: Wild-garlic extracts were tested for spasmolytic activity on isolated rat ileum, antimicrobial activity on selected Gram-positive and Gram-negative bacteria and fungi by microdilution method and antioxidant capacity by DPPH radical-scavenging assay...
May 23, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28542928/crosstalk-between-e2f1-and-p53-transcription-factors-in-doxorubicin-induced-dna-damage-evidence-for-preventive-protective-effects-of-silymarin
#4
Seyedeh-Khadijeh Shafiei-Roudbari, Hassan Malekinejad, Hamed Janbaz-Aciabar, Mazdak Razi
OBJECTIVES: To study the effects of silymarin in various forms of applications on the molecular mechanism(s) of doxorubicin-induced testicular toxicity in male rats. METHODS: Following DOX administration with or without SMN in male rats, sperm quality assays were conducted. Moreover, total antioxidant capacity and nitric oxide content of testis were determined. Expression profile of p53 and E2F1 was analysed by PCR technique. Ultimately, the rate of DNA fragmentation in the testes was quantitatively measured...
May 23, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28542915/effect-of-aqueous-extract-and-anthocyanins-of-calyces-of-hibiscus-sabdariffa-malvaceae-in-rats-with-adenine-induced-chronic-kidney-disease
#5
Badreldin H Ali, Lucie Cahliková, Lubomir Opletal, Turan Karaca, Priyadarsini Manoj, Aishwarya Ramkumar, Yousuf M Al Suleimani, Mohammed Al Za'abi, Abderrahim Nemmar, Lucie Chocholousova-Havlikova, Miroslav Locarek, Tomas Siatka, Gerald Blunden
OBJECTIVES: The aim of this work was to assess the possible beneficial effects of aqueous extracts of Hibiscus sabdariffa L. calyces and anthocyanins isolated therefrom in an adenine-induced chronic kidney disease (CKD) model. METHODS: Rats were orally given, for 28 consecutive days, either adenine alone or together with either aqueous extract of H. sabdariffa calyces (5 and 10%) or anthocyanins (50, 100 and 200 mg/kg of anthocyanin concentrate). For comparative purposes, two groups of rats were given lisinopril (10 mg/kg)...
May 23, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28542812/modulating-nasal-mucosal-permeation-using-metabolic-saturation-and-enzyme-inhibition-techniques
#6
Varsha Dhamankar, Maureen D Donovan
OBJECTIVE: Presystemic elimination resulting from local enzymatic degradation can play a key role in limiting the bioavailability of intranasally administered drugs. The aim of this study was to evaluate the transfer of a metabolically susceptible drug across the nasal mucosa to illustrate the relative contributions of drug diffusivity and metabolic susceptibility on overall nasal mucosal permeation and to understand the effects of changes in enzymatic activity on the transfer across nasal epithelial and submucosal tissues...
May 23, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28523644/elicitation-as-a-tool-to-improve-the-profiles-of-high-value-secondary-metabolites-and-pharmacological-properties-of-hypericum-perforatum
#7
REVIEW
Preeti Shakya, Gregory Marslin, Karthik Siram, Ludger Beerhues, Gregory Franklin
OBJECTIVES: In this review, we aim at updating the available information on the improvement of the Hypericum perforatum L. (Hypericaceae) phytochemical profile and pharmacological properties via elicitation. KEY FINDINGS: Hypericum perforatum seedlings, shoots, roots, calli and cell suspension cultures were treated with diverse elicitors to induce the formation of secondary metabolites. The extracts of the elicitor-treated plant material containing naphthodianthrones, phloroglucinols, xanthones, flavonoids and other new compounds were quantitatively analysed and tested for their bioactivities...
May 19, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28508406/hypericum-perforatum-l-supplementation-protects-sciatic-nerve-injury-induced-apoptotic-inflammatory-and-oxidative-damage-to-muscle-blood-and-brain-in-rats
#8
Fuat Uslusoy, Mustafa Nazıroğlu, İshak Suat Övey, Tolga Taha Sönmez
OBJECTIVES: This study was conducted to explore whether Hypericum perforatum L. (HPL) as a potent antioxidant protects against oxidative stress, cytokine production and caspase expression in muscle (soleus), brain and blood of sciatic nerve injury (SNI)-induced rats. METHODS: Thirty-five rats were equally divided into five groups. The first and second were used as untreated control and sham control groups, respectively. The third, fourth and fifth were sham + HPL, SNI and SNI + HPL groups, respectively...
May 16, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28481011/omega-3-fatty-acids-in-prevention-of-diabetic-retinopathy
#9
REVIEW
Tapan Behl, Anita Kotwani
OBJECTIVES: To review the competence of Omega-3 fatty acids in restricting the progression, thereby leading to prevention of diabetic retinopathy. KEY FINDINGS: Owing to their anti-inflammatory and anti-angiogenic properties, Omega-3 fatty acids alleviate major aetiological agents. These fatty acids are renowned for their beneficial effects in various cardiovascular and other disorders; however, their potential to prevent the progression of diabetic retinopathy remains least explored...
May 8, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28480594/nanostructured-dpa-mpc-dpa-triblock-copolymer-gel-for-controlled-drug-release-of-ketoprofen-and-spironolactone
#10
Bahaa Azmy, Guy Standen, Petra Kristova, Andrew Flint, Andrew L Lewis, Jonathan P Salvage
OBJECTIVE: Uncontrolled rapid release of drugs can reduce their therapeutic efficacy and cause undesirable toxicity; however, controlled release from reservoir materials helps overcome this issue. The aims of this study were to determine the release profiles of ketoprofen and spironolactone from a pH-responsive self-assembling DPA-MPC-DPA triblock copolymer gel and elucidate underlying physiochemical properties. METHODS: Drug release profiles from DPA50 -MPC250 -DPA50 gel (pH 7...
May 7, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28471040/farnesylthiosalicylic-acid-loaded-lipid-polyethylene-glycol-polymer-hybrid-nanoparticles-for-treatment-of-glioblastoma
#11
Abbas Kaffashi, Sevda Lüle, Sibel Bozdağ Pehlivan, Can Sarısözen, İmran Vural, Hüsnü Koşucu, Taner Demir, Kadir Emre Buğdaycı, Figen Söylemezoğlu, Kader Karlı Oğuz, Melike Mut
OBJECTIVES: We aimed to develop lipid-polyethylene glycol (PEG)-polymer hybrid nanoparticles, which have high affinity to tumour tissue with active ingredient, a new generation antineoplastic drug, farnesylthiosalicylic acid (FTA) for treatment of glioblastoma. METHOD: Farnesylthiosalicylic acid-loaded poly(lactic-co-glycolic acid)-1,2 distearoyl-glycerol-3-phospho-ethanolamine-N [methoxy (PEG)-2000] ammonium salt (PLGA-DSPE-PEG) with or without 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP) hybrid nanoparticles has been prepared and evaluated for in-vitro characterization...
May 4, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28471000/encapsulation-of-ritonavir-in-solid-lipid-nanoparticles-in-vitro-anti-hiv-1-activity-using-lentiviral-particles
#12
Farzaneh Javan, Alireza Vatanara, Kayhan Azadmanesh, Mohsen Nabi-Meibodi, Mehdi Shakouri
OBJECTIVES: In this study, ritonavir was entrapped into solid lipid nanoparticles (SLNs) employing two production methods. The prepared SLNs were characterized and antiretroviral activity was investigated for more efficient formulation. METHODS: Ritonavir-loaded SLNs were produced by solvent emulsification evaporation (SE) and double emulsion methods (DE), and the effects of Tween80 and poloxamer188 as external phase surfactant were compared. Prepared SLNs were characterized in terms of size, surface charge, entrapment efficiency (EE), release profile and thermal behaviour...
May 4, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28470967/challenges-for-the-pharmaceutical-technical-development-of-protein-coformulations
#13
REVIEW
Claudia Mueller, Ulrike Altenburger, Silke Mohl
OBJECTIVES: This review discusses challenges to stability, analytics and manufacturing of protein coformulations. Furthermore, general considerations to be taken into account for the pharmaceutical development of coformulated protein drug products are highlighted. KEY FINDINGS: Coformulation of two or more active substances in one single dosage form has recently seen increasing use offering several advantages, such as increased efficacy and/or the overall reduction of adverse event incidents in patients...
May 4, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28464303/phytochemical-and-biological-studies-of-atriplex-inflata-f-muell-isolation-of-secondary-bioactive-metabolites
#14
Aymen Ben Nejma, Mansour Znati, Asma Nguir, Adam Daich, Mohamed Othman, Ata Martin Lawson, Hichem Ben Jannet
OBJECTIVES: This work describes the phytochemical and biological investigation of the Tunisian Atriplex inflata F. Muell (Chenopodiaceae). METHODS: Their chemical structures were elucidated on the basis of extensive spectroscopic methods, including 1D NMR and 2D NMR, ESI-HRMS and comparison with available literature data. The isolates were evaluated for their antioxidant activity by the DPPH(•) , ABTS(+•) , Fe(3+) and catalase assays and also for their antibacterial and anticholinesterase activity...
May 2, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28464236/neuroprotection-by-plumbagin-involves-bdnf-trkb-pi3k-akt-and-erk1-2-jnk-pathways-in-isoflurane-induced-neonatal-rats
#15
Jun-Hui Yuan, Feng Pan, Jie Chen, Cai-Er Chen, Deng-Pan Xie, Xing-Zhu Jiang, Su-Juan Guo, Jun Zhou
OBJECTIVES: This study was designed to assess the effects of plumbagin on isoflurane-induced neurotoxicity. METHODS: Neonatal Sprague Dawley rat pups were treated with plumbagin (50, 100 or 150 mg/kg body weight, orally) from postnatal day 2. The pups on postnatal day 7 were subjected to isoflurane (0.75%) exposure for 6 h. Neuronal apoptosis in the hippocampal tissues was detected by TUNEL assay and FluroJade B staining following isoflurane exposure. Protein expressions were analysed by immunoblotting...
May 2, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28464225/self-assembly-hydrogels-as-multifunctional-drug-delivery-of-paclitaxel-for-synergistic-tumour-targeting-and-biocompatibility-in-vitro-and-in-vivo
#16
Chang Shu, Eboka M B Sabi-Mouka, Xiaoliang Wang, Li Ding
OBJECTIVES: In this work, we designed the self-assembly peptide hydrogels to multiply therapeutic agents for improving anticancer effect and lowering adverse reaction of paclitaxel (PTX). METHODS: The folate (FA)-peptide-PTX hydrogels consist of self-assemble peptide hydrogel as nanoscale carrier, FA and RGD peptide as targeting moieties and paclitaxel as anticancer drug. The properties of hydrogels, such as morphology, size distribution, zeta potential and rheology, were investigated...
May 2, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28447339/activity-of-anti-inflammatory-analgesic-and-antigenotoxic-of-the-aqueous-flower-extracts-of-opuntia-microdasys-lem-pfeiff
#17
Hassiba Chahdoura, Safia El Bok, Taoufik Refifa, Khaoula Adouni, Fethia Khemiss, Habib Mosbah, Mossadok Ben-Attia, Guido Flamini, Lotfi Achour
OBJECTIVES: The aim of this study was to evaluate the analgesic and the anti-inflammatory activity of Opuntia microdasys at post flowering stage, F3 (OMF3) in rat and, in other hand, its antigenotoxic effects by the Allium cepa test. METHODS: OMF3 extracts were screened for activity of analgesic and anti-inflammatory using, respectively, the acetic acid writhing test in mice and the carrageenan-induced paw oedema assay in rats. The antigenotoxic has been evaluated by A...
April 26, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28444868/an-ecological-approach-to-discover-new-bioactive-extracts-and-products-the-case-of-extremophile-plants
#18
Ramla Sahli, Céline Rivière, Christel Neut, Joanne Bero, Marie-Emmanuelle Sahuc, Abderrazak Smaoui, Claire Beaufay, Vincent Roumy, Thierry Hennebelle, Yves Rouillé, Joëlle Quetin-Leclercq, Karin Séron, Riadh Ksouri, Sevser Sahpaz
OBJECTIVES: Eight extremophile plants from Tunisia were screened to find natural products with benefits in human health. METHODS: These plants were collected in different areas in Tunisia. Their methanolic extracts were evaluated for their total phenolic content and for their antiradical (DPPH), antimicrobial (on 35 bacteria and one yeast), antiviral (hepatitis C virus, HCV) and cytotoxic activity (against WI38 and J774 cell lines). The most active species were subjected to a bioguided fractionation...
April 26, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28444771/oestrone-targeted-liposomes-for-mitoxantrone-delivery-via-oestrogen-receptor-synthesis-physicochemical-characterization-and-in-vitro-evaluation
#19
Qiang Hao, Guoxing Xu, Yue Yang, Yuxin Sun, Dengli Cong, Hongrui Li, Xin Liu, Zeng Wang, Zheng Zhang, Jinglin Chen, Yao Li, Xue Luan, Lin Wang, Lin Tian, Kun Liu, Yan Li, Qianru Jiao, Jin Pei
OBJECTIVES: Targeted delivery of mitoxantrone (MTO, an anthraquinone drug with high antitumour effect) may be achieved using a novel nanoparticulate delivery system via binding the oestrogen receptor (ER, highly expressed in a variety of human tumours). METHODS: A novel liposomal nanoparticle (NP) was developed using a conjugate derived from 1, 2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[amino (polyethylene glycol)-2000] (DSPE-PEG2000 -NH2 ) and oestrone (ES, is known to bind the ER) to produce an ES-targeted PEGylated liposome (ES-SSL)...
April 26, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28436532/bis-phenylimidazoselenazolyl-diselenide-elicits-antinociceptive-effect-by-modulating-myeloperoxidase-activity-nox-and-nfkb-levels-in-the-collagen-induced-arthritis-mouse-model
#20
Pietro M Chagas, Bruna C W Fulco, Marcel H M Sari, Juliano A Roehrs, Cristina W Nogueira
Bis(phenylimidazoselenazolyl) diselenide (BPIS) is an organoselenium with acute antinociceptive and antioxidant properties. OBJECTIVES: The aim of this study was to investigate BPIS effect on a collagen-induced arthritis (CIA) model in mice. METHODS: Protocol of exposure consisted in arthritis induction by chicken collagen type II on day 0 with booster injection on day 21. On day 60 after collagen injection, incidence of mechanic allodynia (Von Frey test) or thermal hyperalgesia (hot plate test) was evaluated...
April 24, 2017: Journal of Pharmacy and Pharmacology
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