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https://www.readbyqxmd.com/read/29785666/evaluation-of-ostarine-as-a-selective-androgen-receptor-modulator-in-a-rat-model-of-postmenopausal-osteoporosis
#1
D B Hoffmann, M Komrakova, S Pflug, M von Oertzen, D Saul, L Weiser, T A Walde, M Wassmann, A F Schilling, W Lehmann, S Sehmisch
Selective androgen receptor modulators (SARMs) have shown beneficial effects on muscle wasting, general physical function and bone properties in male mammals. However, data on the effects of SARMs in postmenopausal osteoporotic bone are scarce. We evaluated the effects of the SARM drug ostarine on postmenopausal osteoporotic bone in a rat osteoporosis model. Ovariectomy was performed on 46 of 56 3-month-old female Sprague-Dawley rats. Eight weeks after ovariectomy, ostarine was orally administered daily for 5 weeks in dosages of 0...
May 21, 2018: Journal of Bone and Mineral Metabolism
https://www.readbyqxmd.com/read/29750991/celastrol-attenuates-incision-induced-inflammation-and-pain-associated-with-inhibition-of-the-nf-%C3%AE%C2%BAb-signalling-pathway-via-sarm
#2
Xuhui Chen, Bo Zhang, Jiayan Li, Miaomiao Feng, Yue Zhang, Wenlong Yao, Chuanhan Zhang, Li Wan
AIM: This study aimed to investigate whether celastrol (CEL) could alleviate incision-induced pain and decipher its possible mechanism. MATERIALS AND METHODS: Sprague-Dawley rats were randomly divided into five groups: naïve, vehicle, CEL (5 μg/paw, 10 μg/paw and 20 μg/paw). CEL or vehicle was administered intraplantarly before plantar surgical incision. Histological examinations of skin tissues were performed after HE staining. Additionally, immunohistochemical staining, RT-PCR and western blot were performed to analyse macrophages, proinflammatory cytokines, SARM and NF-κB expression, respectively...
May 8, 2018: Life Sciences
https://www.readbyqxmd.com/read/29746980/in-silico-analysis-of-schmidtea-mediterranea-tir-domain-containing-proteins
#3
Landry Laure Tsoumtsa, Seynabou Sougoufoura, Cedric Torre, Emmanuel Lemichez, Pierre Pontarotti, Eric Ghigo
While genetic evidence points towards an absence of Toll-Like Receptors (TLRs) in Platyhelminthes, the Toll/IL-1 Receptor (TIR)-domains that drive the assembly of signalling complexes downstream TLR are present in these organisms. Here, we undertook the characterisation of the repertoire of TIR-domain containing proteins in Schmidtea mediterranea in order to gain valuable information on TLR evolution in metazoan. We report the presence of twenty proteins containing between one and two TIR domains. In addition, our phylogenetic-based reconstruction approach identified Smed-SARM and Smed-MyD88 as conserved TLR adaptors...
May 7, 2018: Developmental and Comparative Immunology
https://www.readbyqxmd.com/read/29727260/in-house-validation-of-a-liquid-chromatography-tandem-mass-spectrometry-method-for-the-determination-of-selective-androgen-receptor-modulators-sarms-in-bovine-urine
#4
Kathrin S Schmidt, Joachim Mankertz
A sensitive and robust liquid chromatography - tandem mass spectrometry (LC-MS/MS) method allowing the rapid screening and confirmation of selective androgen receptor modulators (SARMS) in bovine urine was developed and successfully validated according to Commission Decision 2002/657/EC, chapter 3.1.3 "alternative validation", by applying a matrix-comprehensive in-house validation concept. The confirmation of the analytes in the validation samples was achieved both on the basis of the multiple reaction monitoring (MRM) ion ratios as laid down in Commission Decision 2002/657/EC and by comparison of their EPI spectra with a reference mass spectral library by making use of the QTRAP technology...
May 4, 2018: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
https://www.readbyqxmd.com/read/29621580/use-of-nutritional-supplements-contaminated-with-banned-doping-substances-by-recreational-adolescent-athletes-in-athens-greece
#5
Konstantinos Tsarouhas, Nassia Kioukia-Fougia, Petros Papalexis, Aristidis Tsatsakis, Dimitrios Kouretas, Flora Bacopoulou, Christina Tsitsimpikou
Although the use of nutritional supplements by adult athletes has been extensively studied, information on supplements consumption by adolescent athletes is still limited. The present study reports on the use of nutritional supplements contaminated with banned doping substances among 170 recreational adolescent athletes from eleven, randomly selected, gym centres, in Athens, Greece. Nutritional supplements consumption was reported by almost 60% of the study population, with proteins/amino acids and vitamins being the most popular...
April 2, 2018: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/29532196/effect-of-gaalas-low-level-laser-therapy-on-mouth-opening-after-orthognathic-surgery
#6
Robson Almeida de Rezende, Daniela Nascimento Silva, Lúcio Frigo
To evaluate low-level laser therapy (LLLT) as an adjunct to enhance postoperative mouth opening after orthognathic surgery. Prospective clinical trial of 82 patients allocated into an intervention group (laser, LG) and a control group (no laser, CG) and subgroups according to the procedure type : (1) surgically assisted rapid maxillary expansion (SARME); (2) maxillary surgery; (3) mandibular surgery; or (4) bimaxillary surgery. LG patients received LLLT immediately after surgery and every 24 h thereafter for 3 days, using a gallium-aluminum-arsenide (GaAlAs) diode laser (780 nm, 28 spots, 14 on each side of the face, output power 2 J/spot)...
March 12, 2018: Lasers in Medical Science
https://www.readbyqxmd.com/read/29527831/development-of-a-selective-androgen-receptor-modulator-for-transdermal-use-in-hypogonadal-patients
#7
V Krishnan, N J Patel, J G Mackrell, S A Sweetana, H Bullock, Y L Ma, T H Waterhouse, B C Yaden, J Henck, Q Q Zeng, K Gavardinas, P Jadhav, A Saeed, P Garcia-Losada, D A Robins, C T Benson
We have identified a non-steroidal selective androgen receptor modulator (SARM), termed LY305, that is bioavailable through a transdermal route of administration while highly cleared via hepatic metabolism to limit parent compound exposure in the liver. Selection of this compound and its transdermal formulation was based on the optimization of skin absorption properties using both in vitro and in vivo skin models that supported PBPK modeling for human PK predictions. This molecule is an agonist in perineal muscle while being a weak partial agonist in the androgenic tissues such as prostate...
March 12, 2018: Andrology
https://www.readbyqxmd.com/read/29521749/root-fracture-as-complication-of-surgically-assisted-rapid-maxillary-expansion
#8
Pedro Henrique de Azambuja Carvalho, Robson Rodrigues Garcia, Cristiane Bonanato Estrela, Valfrido Antônio Pereira Filho
A 23 year old male patient was submitted to surgical assisted rapid maxillary expansion (SARME). There were any postoperative complications until the finish of orthodontic expansion process. However, in the 30th postoperative day, patient mentioned pain in upper central incisor. Periapical radiography evidenced a root fracture of central upper right incisor. After endodontic treatment, the fractured apex was removed. After 3 years of follow-up, the patient finished orthodontics, and the damaged tooth was in good aspect...
March 8, 2018: Journal of Craniofacial Surgery
https://www.readbyqxmd.com/read/29501194/environmentally-friendly-microwave-assisted-sequential-extraction-method-followed-by-icp-oes-and-ion-chromatographic-analysis-for-rapid-determination-of-sulphur-forms-in-coal-samples
#9
Nomvano Mketo, Philiswa N Nomngongo, J Catherine Ngila
A rapid three-step sequential extraction method was developed under microwave radiation followed by inductively coupled plasma-optical emission spectroscopic (ICP-OES) and ion-chromatographic (IC) analysis for the determination of sulphur forms in coal samples. The experimental conditions of the proposed microwave-assisted sequential extraction (MW-ASE) procedure were optimized by using multivariate mathematical tools. Pareto charts generated from 23 full factorial design showed that, extraction time has insignificant effect on the extraction of sulphur species, therefore, all the sequential extraction steps were performed for 5 min...
May 15, 2018: Talanta
https://www.readbyqxmd.com/read/29491216/selective-androgen-receptor-modulator-yk11-up-regulates-osteoblastic-proliferation-and-differentiation-in-mc3t3-e1-cells
#10
Tomofumi Yatsu, Taichi Kusakabe, Keisuke Kato, Yoshio Inouye, Kiyomitsu Nemoto, Yuichiro Kanno
Androgens are key regulators that play a critical role in the male reproductive system and have anabolic effects on bone mineral density and skeletal muscle mass. We have previously reported that YK11 is a novel selective androgen receptor modulator (SARM) and induces myogenic differentiation and selective gene regulation. In this study, we show that treatment of YK11 and dihydrotestosterone (DHT) accelerated cell proliferation and mineralization in MC3T3-E1 mouse osteoblast cells. Further, YK11-treated cells increased osteoblast specific differentiation markers, such as osteoprotegerin and osteocalcin, compared to untreated cells...
2018: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29478034/uk-guidelines-on-oesophageal-dilatation-in-clinical-practice
#11
Sarmed S Sami, Hasan N Haboubi, Yeng Ang, Philip Boger, Pradeep Bhandari, John de Caestecker, Helen Griffiths, Rehan Haidry, Hans-Ulrich Laasch, Praful Patel, Stuart Paterson, Krish Ragunath, Peter Watson, Peter D Siersema, Stephen E Attwood
These are updated guidelines which supersede the original version published in 2004. This work has been endorsed by the Clinical Services and Standards Committee of the British Society of Gastroenterology (BSG) under the auspices of the oesophageal section of the BSG. The original guidelines have undergone extensive revision by the 16 members of the Guideline Development Group with representation from individuals across all relevant disciplines, including the Heartburn Cancer UK charity, a nursing representative and a patient representative...
June 2018: Gut
https://www.readbyqxmd.com/read/29463126/comparative-study-of-internal-fixation-of-the-ulna-and-distal-ulna-resection-in-patients-older-than-70-years-with-distal-radius-and-distal-metaphyseal-ulna-fractures
#12
Jorge G Boretto, Ezequiel E Zaidenberg, Gerardo L Gallucci, Alejandro Sarme, Pablo De Carli
BACKGROUND: Acute management of fractures of the distal ulna that are associated with fractures of the distal radius remains difficult, particularly in the elderly. METHODS: In this study, we investigated whether internal fixation of the distal ulna is associated with a higher rate of complications than resection of the distal ulna in patients older than 70 years. Twenty-four consecutive patients were included in this study, 12 of whom had undergone open reduction and internal fixation (ORIF) of the distal ulna, and 12 who had undergone distal ulna resection...
February 1, 2018: Hand: Official Journal of the American Association for Hand Surgery
https://www.readbyqxmd.com/read/29444261/selective-androgen-receptor-modulator-s42-suppresses-prostate-cancer-cell-proliferation
#13
Takako Kawanami, Tomoko Tanaka, Yuriko Hamaguchi, Takashi Nomiyama, Hajime Nawata, Tosihiko Yanase
We previously identified the selective androgen receptor (AR) modulator S42, which does not stimulate prostate growth but has a beneficial effect on lipid metabolism. In the prostate cancer (PC) cell line LNCaP, S42 did not induce AR transactivation but antagonized 5α-dihydrotestosterone (DHT)‒induced AR activation. Next, we investigated whether S42 suppresses the growth of PC cell lines. Basal growth of LNCaP cells was significantly suppressed by treatment with S42 compared with vehicle, as determined by cell counting and 5-bromo-2'-deoxyuridine assays...
April 1, 2018: Endocrinology
https://www.readbyqxmd.com/read/29430877/detection-of-prohibited-substances-in-equine-hair-by-ultra-high-performance-liquid-chromatography-triple-quadrupole-mass-spectrometry-application-to-doping-control-samples
#14
B Gray, M Viljanto, E Menzies, L Vanhaecke
The detection of drugs in human hair samples has been performed by laboratories around the world for many years and the matrix is popular in disciplines, such as workplace drug testing. To date, however, hair has not become a routinely utilised matrix in sports drug detection. The analysis of hair samples offers several potential advantages to doping control laboratories, not least of which are the greatly extended detection window and the ease of sample collection and storage. This article describes the development, validation, and utilisation of a sensitive ultra-high performance liquid chromatography-triple quadrupole mass spectrometry (UHPLC-MS/MS) method for the detection of 50 compounds...
February 12, 2018: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29411717/evaluation-of-two-different-rapid-maxillary-expansion-surgical-techniques-and-their-effects-on-the-malar-complex-based-on-3d-cone-beam-computed-tomography
#15
P Aktop, S Biren, S Aktop, M Motro, C Delilbasi, G Gurler, G Dergin
We compared and evaluated the effects of two techniques used for surgically assisted rapid maxillary expansion (SARME) using three-dimensional (3D) cone-beam computed tomography, focusing on changes in soft and hard tissue in the malar region. A conventional Le Fort I osteotomy group (10 patients, mean age: 19.3 years) and a high Le Fort I group (12 patients, mean age: 20.4 years) underwent 3D analyses. Changes in hard and soft tissue of the malar region were compared. The average increases in the bone malar width and soft malar width in the high Le Fort I group between the pre- and postoperative periods were 1...
January 2018: Nigerian Journal of Clinical Practice
https://www.readbyqxmd.com/read/29395452/evaluation-of-stress-by-finite-element-analysis-of-the-midface-and-skull-base-at-the-time-of-midpalatal-osteotomy-in-models-with-or-without-pterygomaxillary-dysjunction
#16
A Esen, E Soganci, E Dolanmaz, D Dolanmaz
Surgically-assisted rapid maxillary expansion (SARME) is commonly used to treat skeletally mature patients with transverse discrepancies. Some osteotomies are made in areas that resist expansion, but there is no clear consensus about the sequence in which the osteotomies are made. Some clinicians do the pterygomaxillary osteotomy last, while others do it before the midpalatal osteotomy. We used the finite element method to measure the stresses on the midface, cranial base and pterygoid plates at the time of midpalatal osteotomy in two models, one with and one without pterygomaxillary dysjunction (PMD)...
April 2018: British Journal of Oral & Maxillofacial Surgery
https://www.readbyqxmd.com/read/29344250/prevention-of-body-weight-loss-and-sarcopenia-by-a-novel-selective-androgen-receptor-modulator-in-cancer-cachexia-models
#17
Megumi Morimoto, Katsuji Aikawa, Takahito Hara, Masuo Yamaoka
Cancer cachexia is a syndrome that impairs the quality of life and overall survival of patients, and thus the effectiveness of anticancer agents. There are no effective therapies for cancer cachexia due to the complexity of the syndrome, and insufficient knowledge of its pathogenesis results in difficulty establishing appropriate animal models. Previously, promising results have been obtained in clinical trials using novel agents including the ghrelin receptor agonist anamorelin, and the selective androgen receptor modulator (SARM) enobosarm to treat cachexia in patients with cancer...
December 2017: Oncology Letters
https://www.readbyqxmd.com/read/29334634/equine-in-vivo-derived-metabolites-of-the-sarm-lgd-4033-and-comparison-with-human-and-fungal-metabolites
#18
Annelie Hansson, Heather Knych, Scott Stanley, Emma Berndtson, Liora Jackson, Ulf Bondesson, Mario Thevis, Mikael Hedeland
LGD-4033 has been found in human doping control samples and has the potential for illicit use in racehorses as well. It belongs to the pharmacological class of selective androgen receptor modulators (SARMs) and can stimulate muscle growth, much like anabolic steroids. However, SARMs have shown superior side effect profiles compared to anabolic steroids, which arguably makes them attractive for use by individuals seeking an unfair advantage over their competitors. The purpose of this study was to investigate the metabolites formed from LGD-4033 in the horse in order to find suitable analytical targets for doping controls...
February 1, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29330747/recent-advances-in-screening-for-barrett-s-esophagus
#19
REVIEW
Sarmed S Sami, Prasad G Iyer
OPINION STATEMENT: PURPOSE OF REVIEW: There is a pressing need for effective strategies to halt the increase in both the incidence and mortality of esophageal adenocarcinoma (EAC). Screening for Barrett's esophagus, which is the only known precursor of EAC, remains a ripe area for research, particularly with regard to identifying the target population, screening tools, and management of screen-detected populations. This review aims to explore in depth the rationale for screening for Barrett's esophagus, recent biotechnological advances which may have the potential of making screening feasible, and also highlight the challenges which will have to be overcome in order make screening for BE a realistic prospect...
March 2018: Current Treatment Options in Gastroenterology
https://www.readbyqxmd.com/read/29319101/structural-elucidation-of-major-selective-androgen-receptor-modulator-sarm-metabolites-for-doping-control
#20
Neeraj Garg, Annelie Hansson, Heather K Knych, Scott D Stanley, Mario Thevis, Ulf Bondesson, Mikael Hedeland, Daniel Globisch
Selective androgen receptor modulators (SARMs) are a class of androgen receptor drugs, which have a high potential to be performance enhancers in human and animal sports. Arylpropionamides are one of the major SARM classes and get rapidly metabolized significantly complicating simple detection of misconduct in blood or urine sample analysis. Specific drug-derived metabolites are required as references due to a short half-life of the parent compound but are generally lacking. The difficulty in metabolism studies is the determination of the correct regio and stereoselectivity during metabolic conversion processes...
January 31, 2018: Organic & Biomolecular Chemistry
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