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Zavatti Manuela M Department of Surgical, Medical, Dental and Morphological Sciences with Interest in Transplants, Oncology and Regenerative Medicine, University of Modena and Reggio Emilia, Modena, Italy. Electronic address: - - 2014
This study aims to evaluate the bone regeneration in a rat calvarias critical size bone defect treated with a construct consisting of collagen type I and human amniotic fluid stem cells (AFSCs) after oral administration of phytoestrogen ferutinin. In 12week old male rats (n=10), we performed two symmetric full-thickness cranial ...
Xu Xin-Chen - - 2014
BackgroundPeriodontitis is an inflammatory disease characterized by the loss of connective tissue and alveolar bone. There is an increasing evidence that periodontitis is associated with a number of chronic disease, including osteoporosis. Periodontitis and osteoporosis are both bone destructive diseases and of high prevalence in adult population. Osteoporosis could increase ...
Samir S M SM Departments of Medical Physiology and Clinical Pharmacology, Faculty of Medicine, Mansoura University, Mansoura, Egypt. - - 2014
Osteoporosis is a common health problem. The endocannabinoid pathway has been implicated as an important regulator of bone turnover. Rimonabant is a potent cannabinoid receptor1 (CB1) receptor antagonist with wide therapeutic use as an antiobesity drug that has been withdrawn due to side effects in the form of depression and ...
Li Guan-Wu GW Department of Radiology, Yueyang Hospital affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai 200437, - - 2014
Although the primary target cell of bisphosphonates is the osteoclast, increasing attention is being given to other effector cells influenced by bisphosphonates, such as osteoblasts and marrow adipocytes. Early zoledronic acid (ZA) treatment to ovariectomized (OVX) rats has been found to fully preserve bone microarchitecture over time. However, little is ...
Froberg-Fejko Karen K Bio-Serv, Flemington, - - 2014
Gnawing is an important natural behavior for rodents. Rodents' teeth grow continuously throughout their lives, and gnawing maintains their dental health. In keeping with recommendations of the Guide for the Care and Use of Laboratory Animals, rodents should be provided with enrichment items that encourage gnawing as a natural behavior. ...
Huh Jeong-Eun JE Oriental Medicine Research Center for Bone and Joint Disease, East-West Bone and Joint Research Institute, Kyung Hee University, 149 Sangil-dong, Gangdong-gu, Seoul, 134-727, Republic of - - 2014
Jasin-hwan-gagambang (BHH10), a modified prescription of Jasin-hwan, contains Astragalus membranaceus, Cinnamomum cassia, and Phellodendron amurense, and it has been traditionally used to treat osteoporosis and other inflammatory diseases. In this study, we systematically investigated the protective effects of BHH10 in ovariectomy (OVX)-induced rats. Sprague-Dawley rats were randomly divided into sham ...
Feng Min M Department of Orthopaedics, Second Affiliated Hospital of Medical School, Xi'an Jiaotong University No.157 Xiwu Road, Xi'an, Shaanxi Province, PR - - 2014
The inhibition of bone formation has been suggested to play a central role in the pathogenesis of glucocorticoid-induced osteoporosis (GIOP). Recently, many studies suggested that there may be another mechanism involved in GIOP besides apoptosis. The aim of this study was to investigate the protective effect of Necrostatin-1 on GIOP ...
Yousefnia Hassan H Nuclear Science and Technology Research Institute (NSTRI), Tehran 14395-836, - - 2014
In this work, the absorbed dose to each organ of human for (166)Ho-TTHMP was evaluated based on biodistribution studies in rats by a RADAR method and was compared with (166)Ho-DOTMP as the only clinically used Ho-166 bone marrow ablative agent. The highest absorbed dose for this complex is observed in ...
Klíma K K Institute of Physiology Academy of Sciences of the Czech Republic, Prague, Czech Republic. - - 2014
Stem cells biology is one of the most frequent topic of physiological research of today. Spinal fusion represents common bone biology challenge. It is the indicator of osteoinduction and new bone formation on ectopic model. The purpose of this study was to establish a simple model of spinal fusion based ...
Zhou Jun J Department of Rehabilitation, The First Affiliated Hospital of University of South China, Hengyang, Hunan, People's Republic of - - 2014
To characterise the effects of early and late electroacupuncture (EA) treatment on serum 17β-oestradiol (E2), C-terminal cross-linking telopeptide of type I collagen (CTX-I), bone mineral density (BMD), biomechanical bone strength and mRNA expression of cathepsin K in ovariectomised (OVX) rats. Sixty Sprague-Dawley rats underwent ovariectomy (n=40) or sham surgery (n=20) ...
Zhang Hong-Shi HS Changchun University of Traditional Chinese Medicine, 1035 Boshuo Road, Changchun Net Month National High and New Technology Industry Development District, Changchun, 130117, Jilin, China, - - 2014
The aim of the study was to explore the effect of birdpecking and revolving moxibustion on twelve back shenshu points on the bone metabolism and bone histomorphometry of osteoporosis rats. The 50 female rats of 8 months old that did not pregnant were collected and randomly divided into sham-operation group, model ...
Chapin Robert E RE Developmental and Reproductive Toxicology Center of Expertise, Pfizer Worldwide R&D (WRD), Groton, - - 2014
Treatment-induced epididymal inflammation and granuloma formation is only an occasional problem in preclinical drug development, but it can effectively terminate the development of that candidate molecule. Screening for backup molecules without that toxicity must be performed in animals (generally rats) that requires at least 2 to 3 weeks of in ...
Jedeon Katia K Centre de Recherche des Cordeliers, INSERM UMRS 1138, Laboratory of Molecular Oral Pathophysiology, Paris, F-75006 - - 2014
Bisphenol A (BPA) is a widespread endocrine disrupting chemical (EDC) strongly suspected to have adverse health effects. Numerous tissues and cells are affected by BPA, and we showed recently that BPA targets include ameloblasts and enamel. We therefore investigated the effects of BPA on ameloblasts and the possible involvement of ...
Zefirov T L TL Department of Anatomy, Physiology, and Human Health Protection, Kazan (Volga Region) Federal University, Kazan, Russia, - - 2014
We studied the effect of α2-adrenoceptor stimulation with clonidine on BP and cardiac activity in rats. Variations in BP and chronotropism of the heart were studied in vivo after bolus injection of clonidine. In vitro experiments were performed to evaluate a dose-dependent change in myocardial contractility of the atria and ...
Ma Jing-Yi JY State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing, 100050, - - 2014
FR429, an ellagitannin (a type of polyphenol), is isolated and purified from Polygonum capitatum Buch.-Ham.ex D. Don which is the original herbal medicine of the "Re-Lin-Qing" formula used clinically to treat urinary tract infection in China. FR429 has been investigated for its antitumor potential in tumor-bearing nude mice in vivo, ...
Yoo Hyun-Wook HW Department of Foods & Nutrition, Kookmin University, 77 Jeongneung-ro, Seongbuk-gu, Seoul 136-702, - - 2014
Soy isoflavones are structurally similar to estrogen and bind to estrogen receptors, suggesting that they exhibit estrogenic activities; therefore, they are referred to as phytoestrogens. Fermentation may affect the bioavailability of isoflavones altering soy isoflavone glycosides in the form of aglycones. Thus, this study investigated the effects of fermented soybeans ...
Su Jing J Center for Reproductive Medicine, The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School, Nanjing City, - - 2014
This study was carried out to investigate the impact of tripterygium glycosides (TGs) on ovarian function of female rats in vitro and in vivo. In vitro studies showed that TG induced cells decrease at G1 phase and inhibited cell proliferation in rat granulosa cells. In vivo, female rats were intragastrically ...
Goswami Sumanta K SK Department of Pharmacology, Al-Ameen College of Pharmacy, Bangalore, - - 2014
Herbs have been used as an aphrodisiac since ages. Cinnamomum cassia is an important ingredient of many Ayurvedic formulations to treat male sexual disorder including erectile dysfunction (ED). The objective of the present study was to evaluate erectogenic and aphrodisiac activity of methanol extract of C. cassia bark in young ...
Liu Hongming H Division of Pharmaceutics, College of Pharmacy, Jinan University , Guangzhou , - - 2014
Abstract 1. The natural polyphenol gossypol possesses many therapeutic benefits. Here we aim to determine the elimination pathways of gossypol in vivo and in vitro. 2. Metabolite elucidation of gossypol was performed using UPLC-QTOF/MS coupled with Metabolynx analysis. Clearance of gossypol was evaluated in bile duct cannulated rats and in the single-pass ...
Brocks Dion R DR 2-142H Katz Group Centre for Pharmacy and Health Research, Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, AB T6G 2E1, - - 2014
In-vitro studies were performed to shed light on previous findings that showed increased uptake of cyclosporine A in the kidneys and liver of hyperlipidemic rats, and increased signs of kidney toxicity. Hepatocytes were obtained from rats, cultured, and exposed to a diluted serum from hyperlipidemic rats. Some cells were also ...
Soars Matthew G MG Department of Discovery DMPK, AstraZeneca Charnwood , Bakewell Road, Loughborough, Leicestershire , UK - - 2014
Abstract 1. Optimization of renal clearance is a complex balance between passive and active processes mediated by renal transporters. This work aimed to characterize the interaction of a series of compounds with rat and human organic anion transporters (OATs) and develop quantitative structure-activity relationships (QSARs) to optimize renal clearance. 2. In vitro ...
Lundquist Patrik P AstraZeneca/Uppsala - - 2014
Well established techniques are available to predict in vivo hepatic uptake and metabolism from in vitro data, but predictive models for biliary clearance remain elusive. Several studies have verified the expression and activity of ATP-binding cassette (ABC) efflux transporters central to biliary clearance in freshly isolated rat hepatocytes, raising the ...
Hu Yang Y Immunology and Reproduction Biology Laboratory, Medical School, Nanjing University, Nanjing, China; Jiangsu Key Laboratory of Molecular Medicine, Nanjing University, Nanjing, China; State Key Laboratory of Analytical Chemistry for Life Science, Nanjing University, Nanjing, - - 2014
The estrogenic chemical nonylphenol (NP) and the antiandrogenic agent di-n-butyl phthalate (DBP) are regarded as widespread environmental endocrine disruptors (EDCs) which at high doses in some species of laboratory animals, such as mice and rats, have adverse effects on male reproduction and development. Given the ubiquitous coexistence of various classes ...
Sabatini David D DD Department of Cell Biology, NYU Medical School, New York, New York - - 2014
This protocol describes how to prepare rat liver rough microsomes that contain undegraded membrane-bound polysomes and can function very well in an in vitro translation system. It uses endogenous ribonuclease inhibitor in all steps, avoiding pelleting rough microsomes in all steps and sacrificing good recovery.
Han Yong-Long YL Department of Pharmacy, Shanghai Jiao Tong University Affiliated Sixth People's Hospital, No. 600 Yishan Road, Shanghai 200233, - - 2014
Inhibition of cytochrome P450 (CYP) and P-glycoprotein (P-gp) are regarded as the most frequent and clinically important pharmacokinetic causes among the various possible factors for drug-drug interactions. Scutellarin is a flavonoid which is widely used for the treatment of cardiovascular diseases. In this study, the in vitro inhibitory effects of ...
Li Chun Lei CL Discipline of Oral Diagnosis & Polyclinics, Faculty of Dentistry, The University of Hong Kong, Prince Philip Dental Hospital, 34 Hospital Road, Hong - - 2014
Objective. Technically primates and dogs represent ideal models to investigate diseases characterized by abnormal intracortical remodeling. High expenses and ethical issues, however, restrict the use of those animals in research. Rodent models have been used as alternatives instead, but their value is limited, if none, because these animals lack intracortical ...
Feresin Rafaela G RG Department of Nutrition, Food and Exercise Sciences, Florida State University, Tallahassee, FL 32306, USA ; The Center for Advancing Exercise and Nutrition Research on Aging (CAENRA), Florida State University, Tallahassee, FL 32306, - - 2014
Obesity and osteoporosis are two chronic conditions that have been increasing in prevalence. Despite prior data supporting the positive relationship between body weight and bone mineral density (BMD), recent findings show excess body weight to be detrimental to bone mass, strength, and quality. To evaluate whether obesity would further exacerbate ...
Cotoia Antonella A Department of Medical and Surgical Sciences, University of Foggia, Foggia, - - 2014
The aim of this study was to test the effect of a small volume administration of p-hydroxyphenylpyruvate (pHPP) in a rat model of profound hemorrhagic shock and to assess a possible metabolic mechanism of action of the compound. The results obtained show that hemorrhaged rats treated with 2-4% of the ...
Zhang Guozhe G Department of Traditional Chinese Medicine, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, - - 2013
Kakkalide and irisolidone, the main isoflavones of Flos Puerariae, exhibit a wide spectrum of bioactivities. Intestinal bacteria biotransformation plays an important role in the metabolic pathways of flavones, and is directly related to the bioactivities of the prodrugs after oral administration. To the best of our knowledge, the metabolic pathways ...
Zhao Gang G School of Medicine, Xi'an Jiaotong University, Xi'an, 710061, - - 2013
In this study, a simple and sensitive gas chromatography-mass spectrometry method was developed for the study of bioavailability and protein binding and the metabolism of imperatorin in rat. The results showed that the pharmacokinetics of imperatorin after intravenous and oral administration in rats exhibited linear characteristics. The absolute bioavailability of ...
Nishizato Yohei Y Preclinical Research Laboratories, Dainippon Sumitomo Pharma Co., Ltd. Electronic address: - - 2013
SMP-028 is a new compound for treatment of asthma. Oral administration of SMP-028 to rats was associated with toxicological events in endocrine organs. These events mainly consisted of pathological changes in the adrenal gland, testis, prostate, seminal vesicle, ovaries, and uterus. In this study, we set to clarify whether SMP-028 ...
Sawant Basak Aarti - - 2013
Abstract 1.  In early discovery stages, 2-methyl-N-(2'-(pyrrolidinyl-1-ylsulfonyl)-[1,1'-biphenyl]-4-yl)propan-1-amine (PBPA) demonstrated monoamine oxidase A (MAO-A) and cytochrome P450 (CYP)-mediated clearance. While human liver microsomes predicted low CLb PBPA demonstrated a moderate CLp/F in humans. The plasma pharmacokinetic (PK) of PBPA was characterized by unexpected high inter-individual variability. Hence, a retrospective analysis was ...
Xu Hui - - 2013
Metabolism of salvianolic acid A (SAA) both in vivo and in vitro was investigated in the present study. LC-MS analysis on drug-containing rat bile and the bile sample hydrolyzed by glucuronidase revealed a series of methylated conjugates of SAA and its glucuronides, as well as the predominace of the methylation ...
Sahu Bhanu P - - 2013
The purpose of this study was to develop a nanosuspension of a poorly soluble drug felodipine by nanoprecipitation to achieve superior in vitro dissolution and high oral absorption in vivo in rats. Felodipine nanosuspensions were prepared by precipitation with ultrasonication method using polyvinyl alcohol (PVA) and hydroxy propyl methyl cellulose ...
Sun Min - - 2013
The present study was the first time to investigate the effects of celastrol, derived from Trypterygium wilfordii Hook F. ("Thunder of God Vine"), a traditional Chinese medicine plant, on the metabolism of model probe substrates of CYP isoforms, CYP1A2, CYP2C11, CYP2D6, CYP2E1 and CYP3A2, which are important in the metabolism ...
Jung Eunjae - - 2013
The aim of this study was to investigate the feasibility of transdermal fluoxetine (FX) delivery. The effects of chemical forms (base or salt) and permeation enhancers on in vitro skin permeation of FX were assessed using hairless mouse, rat and human cadaver skin. The optimized formulations from the in vitro ...
Miyamoto Hirotaka - - 2013
The aim of this study was to evaluate the effect of hypothermia on the in-vivo pharmacokinetics of 4-nitrophenol (4NP) using rat liver homogenate and rat liver perfusion system. Rat liver homogenate was incubated with 4NP, which is mainly metabolized by cytochrome P450 2E1, at 37, 34, 32 or 28°C. The ...
Ferreiro Sara F - - 2013
Azaspiracids (AZAs) are marine biotoxins produced by the dinoflagellate Azadinium spinosum that accumulate in several shellfish species. Azaspiracid poisoning episodes have been described in humans due to ingestion of AZA-contaminated seafood. Therefore, the contents of AZA-1, AZA-2 and AZA-3, the best-known analogs of the group, in shellfish destined to human ...
Sha Baoyong - - 2013
Extensive studies have shown that titanium dioxide (TiO2 ) nanomaterials (NMs) can cause toxicity in vitro and in vivo under normal conditions. However, an adverse effect induced by nano-TiO2 in many diseased conditions, typically characterized by oxidative stress (OS), remains unknown. We investigated the toxicity of nano-TiO2 in rat liver ...
Rennison David - - 2013
Norbormide [5-(α-hydroxy-α-2-pyridylbenzyl)-7-(α-2-pyridylbenzylidene)-5-norbornene-2,3-dicarboximide] (NRB), an existing but infrequently used rodenticide, is known to be uniquely toxic to rats but relatively harmless to other rodents and mammals. However, one major drawback of NRB as a viable rodenticide relates to an evolutionary aversion developed by the rat leading to sub-lethal dosing due to ...
Wenthur Cody J CJ Department of Pharmacology, Vanderbilt University Medical Center, Nashville, Tennessee 37232, - - 2013
A multidimensional, iterative parallel synthesis effort identified a series of highly selective mGlu3 NAMs with submicromolar potency and good CNS penetration. Of these, ML337 resulted (mGlu3 IC50 = 593 nM, mGlu2 IC50 >30 μM) with B:P ratios of 0.92 (mouse) to 0.3 (rat). DMPK profiling and shallow SAR led to ...
Zhou Gao - - 2013
ETHNOPHARMACOLOGICAL RELEVANCE: Meconopsis integrifolia (Maxim.) Franch is a high mountain endemic species used as a traditional Tibetan and Mongolian herb to treat hepatitis, pneumonia, and edema. This study aims to investigate the hepatoprotective and antioxidant effects of Meconopsis integrifolia ethanolic extract (MIE) in vitro and in vivo. MATERIALS AND METHODS: ...
Wang Bao-Lian - - 2013
It is valuable to establish a chemical-pharmacokinetic (PK)-pharmacodynamics (PD) fingerprint of traditional Chinese medicine (TCM) for comprehensively understanding the TCM integrated conception and revealing the material foundation. The chemical, metabolic in vitro, and PK/PD in vivo fingerprints of Schisandra chinensis (SC) alcoholic extract were established and comparatively analyzed using HPLC-UV-MS ...
Nakabayashi T - - 2013
AS1924269-00 is a promising orally applicable anticoagulant that inhibits FVIIa but has very low oral absorption. Therefore, in this study, we aimed to develop a prodrug of AS1924269-00, which possesses a carbamate-added amidine functional group, with high membrane permeability. We investigated the pharmacokinetics of the carbamate-type prodrug of AS1924269-00 in ...
Subramanian Murali - - 2013
Intestinal alkaline phosphatases (IALPs) are widely expressed in the brush border of epithelial cells of the intestinal mucosa. Although their physiological role is unclear, they are very significant when it comes to the release of bioactive parent from orally dosed phosphate prodrugs. Such prodrugs can be resistant to cleavage by ...
Nasr Mohamed M Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Helwan University, Cairo, Egypt. - - 2013
The objective of this study was to prepare celecoxib microcrystals using different stabilizers in order to evaluate the influence of microcrystal formulation on the in vitro dissolution rate and in vivo absorption after oral administration of celecoxib in rats. Three celecoxib microcrystals (MC1, MC2, and MC3) were prepared using solvent ...
Chung J Y JY Department of Biochemistry and Molecular Biology, Johns Hopkins University, School of Medicine, Baltimore, Maryland 21205, - - 2013
Translocator protein (TSPO; 18 kDA) is a high-affinity cholesterol-binding protein that is integrally involved in cholesterol transfer from intracellular stores into mitochondria, the rate-determining step in steroid formation. Previous studies have shown that TSPO drug ligands are able to activate steroid production by MA-10 mouse Leydig tumor cells and by ...
Li Kunjie - - 2013
Trantinterol is a novel β(2)-adrenoceptor agonist used for the treatment of asthma. The aim of this study is to identify the metabolites of trantinterol using liquid chromatography tandem mass spectrometry (LC-MS/MS), to isolate the main metabolites, and confirm their structures by nuclear magnetic resonance (NMR). Urine, feces, bile, and blood ...
Guo Jingjing - - 2013
Methoxychlor (MXC) is primarily used as a pesticide and widely present in the environment. The objective of the present study is to investigate the direct effects of MXC and its metabolite 2-bis(p-hydroxyphenyl)-1,1,1-trichloroethane (HPTE) on two isoforms of 11β-hydroxysteroid dehydrogenase (11β-HSD1 and 11β-HSD2) in vitro. Human liver microsome, rat testis microsome ...
El-Gamal Mohammed I - - 2013
Synthesis of a new ester prodrug of olmesartan, olmesartan hexetil (1), is described. It is in vitro stabilities and in vivo pharmacokinetics (PK) were evaluated. It showed high stability in simulated gastric juice, and was rapidly hydrolyzed to olmesartan in rat liver microsomes and rat plasma in vitro. C(max) and ...
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