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Anabolic agents

Ego Seeman, T J Martin
Bone volume, microstructure and its material composition are maintained by bone remodelling, a cellular activity carried out by bone multicellular units (BMUs). BMUs are focally transient teams of osteoclasts and osteoblasts that respectively resorb a volume of old bone and then deposit an equal volume of new bone at the same location. Around the time of menopause, bone remodelling becomes unbalanced and rapid, and an increased number of BMUs deposit less bone than they resorb, resulting in bone loss, a reduction in bone volume and microstructural deterioration...
February 12, 2019: Nature Reviews. Rheumatology
Mohd Yunus Mohd Heikal, Shuid Ahmad Nazrun, Kien Hui Chua, Abd Ghafar Norzana
The proinflammatory cytokines, metalloproteinases family (MMPs), inflammatory mediators PGE2, COX-2 and NO are the most important group of compounds responsible for the loss of metabolic homeostasis of articular cartilage by promoting catabolic and destructive processes in the pathogenesis of osteoarthritis (OA). Stichopus chloronotus, a marine sea cucumber which is rich in n-3 PUFAs and phenolic compound, may exert a favorable influence on the course of the disease. The objective of this study was to investigate the regeneration and anti-inflammatory potential of S...
February 4, 2019: Cytotechnology
E V McCloskey, L A Fitzpatrick, M-Y Hu, G Williams, J A Kanis
We evaluated the efficacy of abaloparatide in women who were at increased risk for fracture, based on CHMP recommended risk thresholds, at the Abaloparatide Comparator Trial In Vertebral Endpoints (ACTIVE) study baseline. Among patients at high risk based on FRAX probabilities, 18 months of abaloparatide significantly decreased risk for all fracture endpoints compared with placebo. PURPOSE: Abaloparatide, a novel anabolic agent for the treatment of postmenopausal osteoporosis, significantly reduced the risk of vertebral and nonvertebral fractures in the ACTIVE study compared with placebo...
February 5, 2019: Archives of Osteoporosis
Ran Marciano, Manu Prasad, Tal Ievy, Sapir Tzadok, Gabriel Leprivier, Moshe Elkabets, Barak Rotblat
Tumor cells utilize glucose to fuel their anabolic needs, including rapid proliferation. However, due to defective vasculature and increased glucose uptake, tumor cells must overcome glucose deprivation. Accordingly, tumor cells depend on cellular pathways promoting survival under such conditions. Targeting these survival mechanisms can thus serve as a new therapeutic strategy in oncology. As such, we sought to identify small-molecule inhibitors which sensitize tumor cells to glucose starvation by high-throughput drug screening in vitro...
January 30, 2019: Cancers
Yuehong Chen, Ronghan Liu, Aubryanna Hettinghouse, Shuya Wang, Gang Liu, Chuan-Ju Liu
BACKGROUND: Teriparatide, a 1-34 fragment of parathyroid hormone (PTH) that maintains most of the biological activities of PTH, has been employed since 2002 as an anabolic agent for osteoporotic individuals who are at high risk of fracture. The purpose of the present review is to provide a systematic summary and timely update on treatment with teriparatide for fracture prevention. METHODS: Electronic databases, including OVID MEDLINE, OVID Embase, and the Cochrane Library, were searched on February 9, 2018, to identify published systematic reviews and meta-analyses addressing treatment with teriparatide for fracture prevention, and A Measurement Tool to Assess Systematic Reviews 2 (AMSTAR 2) was used to assess the quality of included studies...
January 29, 2019: JBJS Reviews
Allyson Sleeman, Jennifer N Clements
Purpose: The efficacy and safety of abaloparatide, a parathyroid hormone-related protein analog for the treatment of osteoporosis in postmenopausal women at high fracture risk, is reviewed. Summary: A MEDLINE search was conducted for full text English-language articles, using the terms abaloparatide, parathyroid hormone, and osteoporosis. Published articles pertinent to the short- and long-term efficacy and safety of abaloparatide among postmenopausal women with osteoporosis were reviewed and summarized...
January 25, 2019: American Journal of Health-system Pharmacy: AJHP
Cheng Cheng, Dolores Shoback
PURPOSE OF REVIEW: Substantial advances have been made in understanding the biological basis of fracture healing. Yet, it is unclear whether the presence of osteoporosis or prior or current osteoporosis therapy influences the healing process or is associated with impaired healing. This review discusses the normal process of fracture healing and the role of osteoporosis and patient-specific factors in relation to fracture repair. RECENT FINDINGS: The definitive association of osteoporosis to impaired fracture healing remains inconclusive because of limited evidence addressing this point...
January 22, 2019: Current Osteoporosis Reports
Feng Wen, Jun Yu, Cheng-Jian He, Zhi-Wen Zhang, Ao-Fei Yang
Increasing cell apoptosis is one of the major causes of intervertebral disc degeneration (IDD). β-ecdysterone has been demonstrated to protect PC12 cells against neurotoxicity. A previous study revealed that β‑ecdysterone may be involved in the regulation of autophagy in osteoblasts. Therefore, we hypothesized that β‑ecdysterone may possess therapeutic effects on IDD via autophagy stimulation. The effect of β‑ecdysterone on IDD was explored by in vitro experiments. The results demonstrated that β‑ecdysterone attenuated the apoptosis induced by tert‑butyl hydroperoxide via promoting autophagy in nucleus pulposus cells...
January 15, 2019: Molecular Medicine Reports
Lucas Moraes Berneira, Samantha Coelho de Freitas, Caroline Carapina da Silva, Alexandre de Mattos Machado, Claudio Martin Pereira de Pereira, Marco Aurélio Ziemann Dos Santos
Over the past ten years, there has been a significant increase in the amount of formulations containing anabolic androgenic steroids apprehended worldwide. A considerable amount of these illicit preparations is falsified imposing a series of challenges for the analytical identification of alleged active ingredients due to the presence of interferers. In this sense, the aim of this work was to identify and quantify the active ingredient using cholesterol as internal standard in eight apprehended formulations of anabolic androgenic steroids in either tablet, capsule or injectable forms employing visual inspection and instrumental analysis of Fourier Transform Infrared Spectroscopy, Gas Chromatography - Mass Spectrometry and Differential Scanning Calorimetry...
January 10, 2019: Forensic Science International
Masakazu Atobe, Takamichi Nagami, Shuji Muramatsu, Takeshi Ohno, Masayuki Kitagawa, Hiroko Suzuki, Masashi Ishiguro, Atsushi Watanabe, Masashi Kawanishi
Osteoarthritis (OA) is a degenerative disease characterized by joint destruction and loss of cartilage. There are many unmet needs in the treatment of OA and there are few promising candidates for disease-modifying OA drugs, particularly anabolic agents. Here, we describe the identification of novel quinazolin-4(3H)-one derivatives which stimulate chondrocyte cartilage matrix production via TRPV4 and mitigate damaged articular cartilage. We successfully identified the water-soluble, highly potent quinazolin-4(3H)-one derivative 36 and studied its intra-articular physicochemical profile to use in in vivo surgical OA model studies...
January 10, 2019: Journal of Medicinal Chemistry
Vinay Kumar, Varsha Shriram, Rani Bhagat, Tushar Khare, Shivanjali Kapse, Narendra Kadoo
Essential oils (EOs) obtained from aerial parts of Pogostemon deccanensis were analyzed for GC-MS profiling, and evaluated for antioxidant, anti-inflammatory, and anti-proliferative activities. GC-MS analysis revealed a total of 47 constituents, establishing the EOs rich in sesquiterpene with > 20 sesquiterpenes constituting around 77% of the total EO yield. Major constituents included Curzerene (Benzofuran, 6-ethenyl-4,5,6,7-tetrahydro-3,6-dimethyl-5-isopropenyl-, trans-) (26.39%) and epi-Cadinol (22...
January 2019: 3 Biotech
Claudio Vernieri, Diego Signorelli, Giulia Galli, Monica Ganzinelli, Massimo Moro, Alessandra Fabbri, Elena Tamborini, Mirko Marabese, Elisa Caiola, Massimo Broggini, Lital Hollander, Rosaria Gallucci, Giulia Vandoni, Cecilia Gavazzi, Tiziana Triulzi, Mario Paolo Colombo, Angela Maria Rizzo, Paola Antonia Corsetto, Giancarlo Pruneri, Filippo de Braud, Gabriella Sozzi, Valter Torri, Marina Chiara Garassino
Advanced lung adenocarcinoma with inactive liver kinase B1 (LKB1) tumor suppressor protein is associated with poor response to immune checkpoint inhibitors and molecularly targeted agents, and with dismal patient prognosis. LKB1 is a central orchestrator of cancer cell metabolism, and halts tumor growth/proliferation during metabolic stress. Recent preclinical evidence suggests that LKB1-inactive lung adenocarcinoma is highly sensitive to metformin, a safe and low-cost antidiabetic compound that inhibits mitochondrial oxidative phosphorylation...
December 19, 2018: Clinical Lung Cancer
Mir Sadat-Ali, Sulliman M AlShammari, Fares Z Uddin, Fawaz M Alani, Omar S Dahduli
OBJECTIVE: The objective of this study was to identify deficiencies in initiating anti-osteoporotic treatment following a fragility femoral fracture. METHODS: All patients ≥55 years of age treated for a fragility femoral fracture between June 2012 and May 2017 were enrolled. Medications at discharge and at 90 days and 1 year of follow up were analyzed. Patients were classified into 4 groups: Group I did not receive any treatment for osteoporosis; Group II received only calcium and vitamin D3 ; Group III received an anabolic agent, calcium, and vitamin D3 ; and Group IV received bisphosphonates, calcium, and vitamin D3 ...
January 7, 2019: Journal of International Medical Research
Jihee Kim, Chad A Grotegut, James W Wisler, Tianyu Li, Lan Mao, Minyong Chen, Wei Chen, Paul B Rosenberg, Howard A Rockman, Robert J Lefkowitz
BACKGROUND: β2 -adrenergic receptors (β2 ARs) are the target of catecholamines and play fundamental roles in cardiovascular, pulmonary, and skeletal muscle physiology. An important action of β2 AR stimulation on skeletal muscle is anabolic growth, which has led to the use of agonists such as clenbuterol by athletes to enhance muscle performance. While previous work has demonstrated that β2 ARs can engage distinct signaling and functional cascades mediated by either G proteins or the multifunctional adaptor protein, β-arrestin, the precise role of β-arrestin in skeletal muscle physiology is not known...
December 27, 2018: Skeletal Muscle
Juhyun Park, Ohseong Kwon, Sung Yong Cho, Min Chul Cho, Jae Seung Paick, Soo Woong Kim
PURPOSE: To compare the improving effects of diabetic erectile dysfunction with two anti-glycemic agents; phlorizin and insulin. MATERIALS AND METHODS: Sixty Sprague-Dawley rats were divided into four groups (n=15 in each group): normal control (C), untreated diabetic rats (D), and diabetic rats treated by phlorizin (P) or insulin (I). Ten weeks after the diabetic induction using an injection of streptozotocin (55 mg/kg), four weeks of diabetic control was conducted...
November 27, 2018: World Journal of Men's Health
Yagiz Yolcu, Mohammed Alvi, Nathan Wanderman, Bayard Carlson, Arjun Sebastian, Mohamad Bydon, Brett Freedman
Teriparatide (Human recombinant Parathyroid Hormone 1-34) is an anabolic agent that is frequently used in patients with osteoporosis and has been extensively investigated with animal model and clinical studies in current literature. The findings from preclinical studies that have investigated the role of teriparatide in animal models are summarized in presented review. Overall, the studies show an improvement in bone mineral density and increased fusion rates for osteoporotic animals undergoing spine fusion with teriparatide use...
December 27, 2018: International Journal of Neuroscience
Panagiotis Anagnostis, Nifon K Gkekas, Michael Potoupnis, Eustathios Kenanidis, Eleftherios Tsiridis, Dimitrios G Goulis
New anti-osteoporotic agents have been developed, potentially enriching the therapeutic armamentarium. Currently available osteoanabolic therapies are the parathyroid hormone (PTH) and PTH-related peptide (PTHrP) synthetic analogues, teriparatide and abaloparatide. Daily administration at doses of 20 and 80 μg, respectively, in contrast to continuous PTH secretion, leads to increased bone formation and reduces vertebral and non-vertebral fracture risk. Teriparatide is more effective than bisphosphonates (alendronate, risedronate) in increasing bone mineral density (BMD), improving bone architecture and reducing fracture risk...
February 2019: Maturitas
Vidhu Thaker, Ben Carter, Melissa Putman
BACKGROUND: Cystic fibrosis (CF) is an inherited condition causing disease most noticeably in the lungs, digestive tract and pancreas. People with CF often have malnutrition and growth delay. Adequate nutritional supplementation does not improve growth optimally and hence an anabolic agent, recombinant human growth hormone (rhGH), has been proposed as a potential intervention. This is an update of a previously published review. OBJECTIVES: To evaluate the effectiveness and safety of rhGH therapy in improving lung function, quality of life and clinical status of children and young adults with CF...
December 17, 2018: Cochrane Database of Systematic Reviews
Tomas K Kuprys, Leah M Steinmetz, Charla R Fischer, Themistocles S Protopsaltis, Peter G Passias, Jeffrey A Goldstein, John A Bendo, Thomas J Errico, Aaron J Buckland
STUDY DESIGN: Retrospective cohort study. OBJECTIVE: The goals of this study were to (1) evaluate pre-operative bone quality assessment and intervention practice over time and (2) review the current evidence for bone evaluation in spine fusion surgery. SUMMARY OF BACKGROUND DATA: Deformity spine surgery has demonstrated improved quality of life in patients however its cost has made it controversial. If pre-operative bone quality can be optimized then potentially these treatments could be more durable however, at present, no clinical practice guidelines have been published by professional spine surgical organizations...
December 11, 2018: Spine
Caiwei Wang, Li Yan, Bo Yan, Li Zhou, Wan Sun, Lingying Yu, Fucun Liu, Wenxi Du, Guangping Yu, Zhengyan Hu, Qiang Yuan, Luwei Xiao, Hongwen Li, Peijian Tong, Jida Zhang, Letian Shan, Thomas Efferth
ETHNOPHARMACOLOGICAL RELEVANCE: Osteoarthritis (OA), characterized by joint pain and cartilage degradation, is the most common form of joint disease worldwide but with no satisfactory therapy available. The ethanol extract of Agkistrodon acutus (EAA) has been widely used as a traditional Chinese medicine (TCM) for the treatment of arthralgia and inflammatory diseases, but there is no report regarding its efficacy on OA to date. Here, we determined the effects of EAA on the pain behavior and cartilage degradation in vivo and clarified its target genes and proteins associated with chondrocyte hypertrophy and apoptosis in vitro...
December 5, 2018: Journal of Ethnopharmacology
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