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Nuclear pharmaceutical

Yixiao Guo, Yao Li, Yidian Yang, Shiyi Tang, Yufan Zhang, Liqin Xiong
Brown adipose tissue (BAT) has been identified as a promising target for the treatment of obesity, diabetes, and relevant metabolism disorders because of the adaptive thermogenesis ability of this tissue. Visualizing BAT may provide an essential tool for pathology study, drug screening, and efficacy evaluation. Owing to limitations of current nuclear and magnetic resonance imaging approaches for BAT detection, fluorescence imaging has advantages in large-scale preclinical research on small animals. Here, fast BAT imaging in mice is conducted based on polymer dots as fluorescent probes...
June 12, 2018: ACS Applied Materials & Interfaces
Margot Schlusselhuber, Justine Godard, Muriel Sebban, Benoit Bernay, David Garon, Virginie Seguin, Hassan Oulyadi, Nathalie Desmasures
Biosurfactants such as lipopeptides are amphiphilic compounds produced by microorganisms such as bacteria of the genera of Pseudomonas and Bacillus . Some of these molecules proved to have interesting antimicrobial, antiviral, insecticide, and/or tensioactive properties that are potentially useful for the agricultural, chemical, food, and pharmaceutical industries. Raw milk provides a physicochemical environment that is favorable to the multiplication of a broad spectrum of microorganisms. Among them, psychrotrophic bacterial species, especially members of the genus Pseudomonas , are predominant and colonize milk during cold storage and/or processing...
2018: Frontiers in Microbiology
Vidushi Mahajan, Rekha Chouhan, Surinder Kitchlu, Kushal Bindu, Sushma Koul, Bikarma Singh, Yashbir S Bedi, Sumit G Gandhi
Genetic diversity is essential for survival and adaptation of high altitude plants such as those of Tanacetum genus, which are constantly exposed to environmental stress. We collected flowering shoots of ten accessions of Tanacetum gracile Hook.f. & Thomson (Asteraceae) (Tg 1-Tg 10), from different regions of cold desert of Western Himalaya. Chemical profile of the constituents, as inferred from GC-MS, exhibited considerable variability. Percentage yield of essential oil ranged from 0.2 to 0.75% (dry-weight basis) amongst different accessions...
June 2018: 3 Biotech
Georgia Melagraki, Georgios Leonis, Evangelos Ntougkos, Vagelis Rinotas, Christos Papaneophytou, Thomas Mavromoustakos, George Kontopidis, Eleni Douni, George Kollias, Antreas Afantitis
The overexpression of Tumor Necrosis Factor (TNF) is directly related to the development of several autoimmune diseases, such as rheumatoid and psoriatic arthritis, inflammatory bowel disease, Crohn's disease, refractory asthma, and multiple sclerosis. Receptor activator of nuclear factor kappa-B ligand (RANKL) belongs to the TNF family, and is the primary mediator of osteoclast-induced bone resorption through interaction with its receptor RANK. The function of RANKL is physiologically inhibited by the action of osteoprotegerin (OPG), which is a decoy receptor that binds to RANKL and prevents the process of osteoclastogenesis...
June 6, 2018: Current Topics in Medicinal Chemistry
Ankit Parikh, Krishna Kathawala, Yunmei Song, Xin-Fu Zhou, Sanjay Garg
Curcumin (CUR) is considered as one of the most bioactive molecules ever discovered from nature due to its proven anti-inflammatory and antioxidant in both preclinical and clinical studies. Despite its proven safety and efficacy, the clinical translation of CUR into a useful therapeutic agent is still limited due to its poor oral bioavailability. To overcome its limitation and enhance oral bioavailability by improving its aqueous solubility, stability, and intestinal permeability, a novel CUR formulation (NCF) was developed using the self-nanomicellizing solid dispersion strategy...
May 29, 2018: Drug Delivery and Translational Research
Pradeep Paudel, Hyun Ah Jung, Jae Sue Choi
Cassia obtusifolia L. seed is one of the most popular traditional Chinese medicine for mutagenicity, genotoxicity, hepatotoxicity, and acute inflammatory diseases. We evaluated the hepatoprotective activity of anthraquinone and naphthopyrone glycosides isolated from the butanol fraction of C. obtusifolia seeds and explored their effects on cell signaling pathways. Continuous chromatographic separation led to the isolation of 1-desmethylaurantio-obtusin 2-O-β-D-glucopyranoside (1), rubrofusarin 6-O-β-D-apiofuranosyl-(1 → 6)-O-β-D-glucopyranoside (2) and rubrofusarin 6-O-β-gentiobioside (3)...
May 26, 2018: Archives of Pharmacal Research
Mingyan Zhang, Zhibin Yan, Lili Bu, Chunmei An, Dan Wang, Xin Liu, Jianfeng Zhang, Wenle Yang, Bochuan Deng, Junqiu Xie, Bangzhi Zhang
Introduction: Kidney fibrosis is the main pathologic change in diabetic nephropathy (DN), which is the major cause of end-stage renal disease. Current therapeutic strategies slow down but cannot reverse the progression of renal dysfunction in DN. Plant-derived bioactive peptides in foodstuffs are widely used in many fields because of their potential pharmaceutical and nutraceutical benefits. However, this type of peptide has not yet been studied in renal fibrosis of DN. Previous studies have indicated that the peptide YWDHNNPQIR (named RAP), a natural peptide derived from rapeseed protein, has an antioxidative stress effect...
2018: Drug Design, Development and Therapy
Hiroshi Matsuda, Tomoya Uehara, Hidehiko Okazawa, Sunao Mizumura, Kunihiko Yokoyama, Mana Yoshimura
This survey was performed to investigate the incidence of adverse reactions to radiopharmaceuticals in FY2016 in Japan. It was based on responses to questionnaires sent to nuclear medicine institutions. The reply was obtained from 977 institutions among 1,235 to which the questionnaire had been sent. Nine cases of adverse reactions were reported. A total of 1,052,650 radiopharmaceutical administrations was reported. The incidence of adverse reactions per 100,000 cases was 0.9. No case of deficient products was reported...
2018: Kaku Igaku. the Japanese Journal of Nuclear Medicine
S Castellani, A Trapani, A Spagnoletta, L di Toma, T Magrone, S Di Gioia, D Mandracchia, G Trapani, E Jirillo, M Conese
BACKGROUND: Chronic respiratory diseases, whose one of the hallmarks is oxidative stress, are still incurable and need novel therapeutic tools and pharmaceutical agents. The phenolic compounds contained in grape are endowed with well-recognized anti-oxidant, anti-inflammatory, anti-cancer, and anti-aging activities. Considering that natural anti-oxidants, such as proanthocyanidins, have poor water solubility and oral bioavailability, we have developed a drug delivery system based on solid lipid nanoparticles (SLN), apt to encapsulate grape seed extract (GSE), containing proanthocyanidins...
May 23, 2018: Journal of Translational Medicine
Ivana Klopčič, Tijana Markovič, Irena Mlinarič-Raščan, Marija Sollner Dolenc
A critical literature review reveals that knowledge of side effects of pharmaceuticals diclofenac and paracetamol is extremely important because of their widespread use and occurrence in the environment. In order to delineate whether these compounds have endocrine activity and influence on the immune system, we assessed the potential endocrine disrupting and immunomodulatory activities of: diclofenac (DIC), its metabolite 4-hydroxydiclofenac (4-HD) and paracetamol (PAR). Herein, we report on their impact on estrogen receptor (ER), androgen receptor (AR), glucocorticoid receptor (GR) and thyroid hormone receptor (TR)...
May 16, 2018: Toxicology Letters
Ryo Nitta, Tsuyoshi Imasaki, Eriko Nitta
The recent 'resolution revolution' in structural analyses of cryo-electron microscopy (cryo-EM) has drastically changed the research strategy for structural biology. In addition to X-ray crystallography and nuclear magnetic resonance spectroscopy, cryo-EM has achieved the structural analysis of biological molecules at near-atomic resolution, resulting in the Nobel Prize in Chemistry 2017. The effect of this revolution has spread within the biology and medical science fields affecting everything from basic research to pharmaceutical development by visualizing atomic structure...
May 16, 2018: Microscopy
Aram Minas, Gholamreza Najafi, Ali Shalizar Jalali, Mazdak Razi
Foeniculum vulgare (FVE; fennel) is an aromatic plant belonging to Umbelliferae family, which is widely used in traditional societies because of its different pharmaceutical properties. To uncover the fennel-derived essential oil (FVEO)-induced effects on male reproductive potential, 24 mature male albino mice were divided into, control, 0.37, 0.75, and 1.5 mg kg-1 FVEO-received groups. Following 35 days, the animals were euthanized and the testicular tissue and sperm samples were collected. The histological alterations, tubular differentiation (TDI), spermiogenesis (SPI) indices, apoptosis ratio, and RNA damage of germinal cells were analyzed...
May 15, 2018: Environmental Toxicology
Un-Ho Jin, Keshav Karki, Sang-Bae Kim, Stephen Safe
Several aryl hydrocarbon receptor (AhR)-active pharmaceuticals were screened as inhibitors of pancreatic cancer cell invasion and identified two compounds, omeprazole, that inhibited invasion. Inhibition of highly invasive Panc1 cell invasion by omeprazole involves an AhR-dependent non-genomic pathway, and omeprazole-mediated inhibition of Panc1 cell invasion was dependent on Jun-N-terminal kinase (JNK) and mitogen-activated kinase kinase 7 (MKK7). The failure of omeprazole to induce nuclear translocation of the AhR was not due to overexpression of cytosolic AhR partner proteins Hsp90 or XAP2, and results of DNA sequencing show that the AhR expressed in Panc1 cells was not mutated...
May 11, 2018: Biochemical and Biophysical Research Communications
Claudia Garnero, Ana Karina Chattah, Carolina Aloisio, Luis Fabietti, Marcela Longhi
Norfloxacin, an antibiotic that exists in different solid forms, has very unfavorable properties in terms of solubility and stability. Binary complexes of norfloxacin, in the solid form C, and β-cyclodextrin were procured by the kneading method and physical mixture. Their effect on the solubility, the dissolution rate, and the chemical and physical stability of norfloxacin was evaluated. To perform stability studies, the solid samples were stored under accelerated storage conditions, for a period of 6 months...
May 10, 2018: AAPS PharmSciTech
Maude Reggane, Johannes Wiest, Marco Saedtler, Cornelius Harlacher, Marcus Gutmann, Sven H Zottnick, Philippe Piechon, Ina Dix, Klaus Müller-Buschbaum, Ulrike Holzgrabe, Lorenz Meinel, Bruno Galli
Realizing the full potential of co-crystals enhanced kinetic solubility demands a comprehensive understanding of the mechanisms of dissolution, phase conversion, nucleation and crystal growth, and of the complex interplay between the active pharmaceutical ingredient (API), the coformer and co-existing forms in aqueous media. One blueprint provided by nature to keep poorly water-soluble bases in solution is the complexation with phenolic acids. Consequently, we followed a bioinspired strategy for the engineering of co-crystals of a poorly water-soluble molecule - Imatinib - with a phenolic acid, syringic acid (SYA)...
May 4, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Geoffrey M Currie
Pharmacology principles provide key understanding that underpins the clinical and research roles of nuclear medicine practitioners. This article is the second in a series of articles that aims to enhance the understanding of pharmacological principles relevant to nuclear medicine. This article will build on the introductory concepts, terminology and principles of pharmacodynamics explored in the first article in the series. Specifically, this article will focus on the basic principles associated with pharmacokinetics...
May 3, 2018: Journal of Nuclear Medicine Technology
Edward Grimley, Gregory R Dressler
Pax genes encode developmental regulators that are expressed in a variety of tissues and control critical events in morphogenesis. In the kidney, Pax2 and Pax8 are expressed in embryonic development and in specific renal diseases associated with aberrant epithelial cell proliferation. Prior genetic and cell biological studies suggest that reducing the activity of Pax proteins in renal cancer or in polycystic kidney disease can slow the progression of these conditions. The Pax proteins may be critical for providing tissue and locus specificity to recruit epigenetic modifiers that control gene expression and chromatin structure...
April 20, 2018: Kidney International
Yuanhang Ma, Qimeng Wang, Kun Yu, Xin Fan, Weidong Xiao, Yujiao Cai, Pengyuan Xu, Min Yu, Hua Yang
6-Formylindolo(3,2-b)carbazole (FICZ), a high-affinity aryl hydrocarbon receptor (AhR) ligand, plays a protective role in inflammatory bowel disease (IBD) through activation of AhR. Interleukin-6 (IL-6) induced intestinal epithelial barrier dysfunction is involved in the pathological process of IBD. In this study, we investigated the protective effects of FICZ on IL-6 induced intestinal epithelial barrier injury. Our data show that AhR activation by FICZ ameliorated colonic inflammation, decreased IL-6 and claudin-2 expression, and maintained intestinal barrier function in a mouse model of dextran sulphate sodium (DSS)-induced colitis...
May 25, 2018: Chemico-biological Interactions
Eun-A Kim, Seo-Young Kim, Bo-Ram Ye, Junseong Kim, Seok-Chun Ko, Won Woo Lee, Kil-Nam Kim, Il-Whan Choi, Won-Kyo Jung, Soo-Jin Heo
In this study, we confirmed the anti-inflammatory effect of Apo-9-fucoxanthinone (AF) in in vitro RAW 264.7 cells and in vivo zebrafish model. In lipopolysaccharide (LPS)-stimulated zebrafish, AF significantly decreased the production of reactive oxygen species (ROS), nitric oxide (NO) and cell death. In addition, the mRNA expression of inducible nitric oxide synthase (iNOS), suppressed cyclooxygenase-2 (COX-2) and an inflammatory cytokines; IL-1β, TNF-α were shown reduction. And AF significantly inhibited NO production and expression of iNOS in LPS-stimulated RAW 264...
June 2018: International Immunopharmacology
Larissa H R Meira, Guilherme A B Soares, Homero I M Bonomini, Juliana Fedoce Lopes, Frederico B De Sousa
Supramolecular structures based on cyclodextrins have been extensively used for drug delivery systems over decades. However, combining host and guest molecules in a pharmaceutical formulation is not a trivial process, being one of the majors concern the inclusion complex compatibility with other excipients presented in the final formulation. Herein, experimental and theoretical calculations were used to investigate the competition of sodium dodecyl sulfate (SDS) with atenolol (ATE) or losartan (LOS), antihypertensive drugs widely used in the treatment of hypertension...
June 10, 2018: International Journal of Pharmaceutics
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