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https://www.readbyqxmd.com/read/28793321/effects-of-combination-treatment-with-alendronate-and-raloxifene-on-skeletal-properties-in-a-beagle-dog-model
#1
Matthew R Allen, Erin McNerny, Mohammad Aref, Jason M Organ, Christopher L Newman, Brian McGowan, Tim Jang, David B Burr, Drew M Brown, Max Hammond, Paul R Territo, Chen Lin, Scott Persohn, Lei Jiang, Amanda A Riley, Brian P McCarthy, Gary D Hutchins, Joseph M Wallace
A growing number of studies have investigated combination treatment as an approach to treat bone disease. The goal of this study was to investigate the combination of alendronate and raloxifene with a particular focus on mechanical properties. To achieve this goal we utilized a large animal model, the beagle dog, used previously by our laboratory to study both alendronate and raloxifene monotherapies. Forty-eight skeletally mature female beagles (1-2 years old) received daily oral treatment: saline vehicle (VEH), alendronate (ALN), raloxifene (RAL) or both ALN and RAL...
2017: PloS One
https://www.readbyqxmd.com/read/28770521/styrene-maleic-acid-encapsulated-raloxifene-micelles-for-management-of-inflammatory-bowel-disease
#2
Khaled Greish, Safa Taha, Anfal Jasim, Sara Abd Elghany, Ameera Sultan, Ali AlKhateeb, Manal Othman, Fang Jun, Sebastien Taurin, Moiz Bakhiet
BACKGROUND: Inflammatory bowel disease (IBD) comprises a group of disorders that manifest through chronic inflammation of the colon and small intestine. Although the exact cause of IBD is still unclear, dysfunctional immunoregulation involving overproduction of inflammatory cytokines such as TNF-α, and IL-6 have been implicated in pathogenesis. Current therapy relies on immunosuppression, cytotoxic drugs, and monoclonal antibodies against TNF-α. These classes of drugs have severe side-effects, especially when used for long duration...
December 2017: Clinical and Translational Medicine
https://www.readbyqxmd.com/read/28770019/cardioprotective-effect-of-selective-estrogen-receptor-modulator-raloxifene-are-mediated-by-heme-oxygenase-in-estrogen-deficient-rat
#3
Anikó Posa, Renáta Szabó, Krisztina Kupai, Anikó Magyariné Berkó, Médea Veszelka, Gergő Szűcs, Denise Börzsei, Mariann Gyöngyösi, Imre Pávó, Zoltán Deim, Zoltán Szilvássy, Béla Juhász, Csaba Varga
Estrogens and raloxifene (RAL) have beneficial effects on certain cardiovascular indices in postmenopausal women characterized by estrogen deficiency. Heme oxygenase (HO) activity is increased by 17β-estradiol (E2) and RAL in estrogen-deficient rat resulting in vasorelaxation mediated by carbon monoxide. We determined the expressions of HO in cardiac and aortic tissues after ovariectomy (OVX) and subsequent RAL or E2 treatment. We investigated the effects of pharmacological inhibition of HO enzyme on the arginine vasopressin- (AVP-) induced blood pressure in vivo, the epinephrine- and phentolamine-induced electrocardiogram ST segment changes in vivo, and the myeloperoxidase (MPO) enzyme activity...
2017: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/28765269/the-efficacy-and-safety-of-vertebral-fracture-prevention-therapies-in-post-menopausal-osteoporosis-treatment-which-therapies-work-best-a-network-meta-analysis
#4
G Wang, L Sui, P Gai, G Li, X Qi, X Jiang
OBJECTIVES: Osteoporosis has become an increasing concern for older people as it may potentially lead to osteoporotic fractures. This study is designed to assess the efficacy and safety of ten therapies for post-menopausal women using network meta-analysis. METHODS: We conducted a systematic search in several databases, including PubMed and Embase. A random-effects model was employed and results were assessed by the odds ratio (OR) and corresponding 95% confidence intervals (CI)...
July 2017: Bone & Joint Research
https://www.readbyqxmd.com/read/28711499/inhibition-of-il-6-stat3-signaling-in-human-cancer-cells-using-evista
#5
Wei Shi, Dan Yan, Chongqiang Zhao, Miaomiao Xiao, Yina Wang, Haiyan Ma, Tianshu Liu, Hua Qin, Cuntai Zhang, Chenglong Li, Jiayuh Lin, Sheng Li, Jiagao Lv, Li Lin
Persistent activation of IL-6/STAT3 signaling pathway has been frequently detected in human cancer including breast cancer, colon cancer and multiple myeloma. IL-6/STAT3 can be a promising target for cancer prevent and treatment. However, few STAT3 inhibitors with high efficiency, specificity and safety is available for present clinical cancer therapy. Evista (Raloxifene·HCl) is known as selective estrogen receptor modulator which has been used for the prevention and treatment of osteoporosis and was approved for reducing the risk of invasive breast cancer...
July 12, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28645573/evidence-that-fetal-death-is-associated-with-placental-aging
#6
Kaushik Maiti, Zakia Sultana, Robert J Aitken, Jonathan Morris, Felicity Park, Bronwyn Andrew, Simon C Riley, Roger Smith
BACKGROUND: The risk of unexplained fetal death or stillbirth increases late in pregnancy, suggesting that placental aging is an etiological factor. Aging is associated with oxidative damage to DNA, RNA, and lipids. We hypothesized that placentas at >41 completed weeks of gestation (late-term) would show changes consistent with aging that would also be present in placentas associated with stillbirths. OBJECTIVE: We sought to determine whether placentas from late-term pregnancies and unexplained stillbirth show oxidative damage and other biochemical signs of aging...
June 20, 2017: American Journal of Obstetrics and Gynecology
https://www.readbyqxmd.com/read/28637206/improving-combination-osteoporosis-therapy-in-a-preclinical-model-of-heightened-osteoanabolism
#7
Yu Shao, Selene Hernandez-Buquer, Paul Childress, Keith R Stayrook, Marta B Alvarez, Hannah Davis, Lilian Plotkin, Yongzheng He, Keith W Condon, David B Burr, Stuart J Warden, Alexander G Robling, Feng-Chun Yang, Ronald C Wek, Matthew R Allen, Joseph P Bidwell
Combining anti-catabolic agents with parathyroid hormone (PTH) to enhance bone mass has yielded mixed results in osteoporosis patients. Towards the goal of enhancing the efficacy of these regimens, we tested their utility in combination with loss of the transcription factor Nmp4 since disabling this gene amplifies PTH-induced increases in trabecular bone in mice by boosting osteoblast secretory activity. We addressed whether combining a sustained anabolic response with an anti-catabolic results in superior bone acquisition compared to PTH mono-therapy...
June 20, 2017: Endocrinology
https://www.readbyqxmd.com/read/28591668/the-selective-estrogen-receptor-modulators-serms-raloxifene-and-tamoxifen-improve-anp-levels-and-decrease-nuclear-translocation-of-nf-kb-in-estrogen-deficient-rats
#8
Aline Z Lamas, Andrews M Nascimento, Ana Raquel S Medeiros, Izabela F Caliman, Polyana L M Dalpiaz, Luciana B Firmes, Glauciene J Sousa, Phablo Wendell C Oliveira, Tadeu U Andrade, Adelina M Reis, Sônia A Gouvea, Nazaré S Bissoli
BACKGROUND: The selective estrogen receptor modulators (SERMs) raloxifene and tamoxifen are used for the treatment of osteoporosis and cancer, respectively, in women. The impairment of both the Atrial Natriuretic Peptide (ANP) cell signaling system and the translocation of nuclear factor-kappa B (NF-kB) to the cell nucleus are associated with detrimental cardiovascular effects and inflammation. The effects of SERMs on these parameters in the cardiac tissue of estrogen-deficient rats has not been reported...
March 16, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28585410/2017-american-college-of-rheumatology-guideline-for-the-prevention-and-treatment-of-glucocorticoid-induced-osteoporosis
#9
Lenore Buckley, Gordon Guyatt, Howard A Fink, Michael Cannon, Jennifer Grossman, Karen E Hansen, Mary Beth Humphrey, Nancy E Lane, Marina Magrey, Marc Miller, Lake Morrison, Madhumathi Rao, Angela Byun Robinson, Sumona Saha, Susan Wolver, Raveendhara R Bannuru, Elizaveta Vaysbrot, Mikala Osani, Marat Turgunbaev, Amy S Miller, Timothy McAlindon
OBJECTIVE: To develop recommendations for prevention and treatment of glucocorticoid-induced osteoporosis (GIOP). METHODS: We conducted a systematic review to synthesize the evidence for the benefits and harms of GIOP prevention and treatment options. The Grading of Recommendations Assessment, Development and Evaluation methodology was used to rate the quality of evidence. We used a group consensus process to determine the final recommendations and grade their strength...
August 2017: Arthritis Care & Research
https://www.readbyqxmd.com/read/28585373/2017-american-college-of-rheumatology-guideline-for-the-prevention-and-treatment-of-glucocorticoid-induced-osteoporosis
#10
Lenore Buckley, Gordon Guyatt, Howard A Fink, Michael Cannon, Jennifer Grossman, Karen E Hansen, Mary Beth Humphrey, Nancy E Lane, Marina Magrey, Marc Miller, Lake Morrison, Madhumathi Rao, Angela Byun Robinson, Sumona Saha, Susan Wolver, Raveendhara R Bannuru, Elizaveta Vaysbrot, Mikala Osani, Marat Turgunbaev, Amy S Miller, Timothy McAlindon
OBJECTIVE: To develop recommendations for prevention and treatment of glucocorticoid-induced osteoporosis (GIOP). METHODS: We conducted a systematic review to synthesize the evidence for the benefits and harms of GIOP prevention and treatment options. The Grading of Recommendations Assessment, Development and Evaluation methodology was used to rate the quality of evidence. We used a group consensus process to determine the final recommendations and grade their strength...
June 6, 2017: Arthritis & Rheumatology
https://www.readbyqxmd.com/read/28576026/design-characterization-and-in-vitro-evaluation-of-novel-amphiphilic-block-sunflower-oil-based-polyol-nanocarrier-as-a-potential-delivery-system-raloxifene-hydrochloride-as-a-model
#11
Niloofar Babanejad, Abdolreza Farhadian, Ismail Omrani, Mohammad Reza Nabid
Presently, modern pharmaceuticals, are almost exclusively derived from the arduous refining of petroleum whose supply is inherently unsustainable. In order to address this issue bio-based materials are increasingly being used for chemical synthesis, particularly in drug delivery systems. Biodegradable and biocompatible hyper-branched polyol (an alcohol containing three or more hydroxyl groups) was synthesized via a facile method through the ring-opening and thiol-ene click reactions at room temperature. Due to the bio-based content of the polyol backbone, the synthesized polyol had both excellent biodegradability and low cytotoxicity...
September 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28541645/raloxifene-plus-antipsychotics-versus-placebo-plus-antipsychotics-in-severely-ill-decompensated-postmenopausal-women-with-schizophrenia-or-schizoaffective-disorder-a-randomized-controlled-trial
#12
Mark Weiser, Linda Levi, Shimon Burshtein, Michal Hagin, Valentin P Matei, Delia Podea, Ioana Micluția, Alexandru Tiugan, Bogdan Păcală, Iosif Gabos Grecu, Adam Noy, Daisy Zamora, John M Davis
OBJECTIVE: Several single-center studies have found raloxifene, an estrogen agonist, to be effective in ameliorating symptoms of schizophrenia in stable patients as augmentation of antipsychotics. This multicenter study assessed whether raloxifene plus antipsychotic treatment, in comparison to placebo plus antipsychotics, improves symptoms or cognition in severely ill decompensated schizophrenia patients. METHODS: In this 16-week, double-blind, randomized, placebo-controlled study, 200 severely ill, decompensated postmenopausal women who met DSM-IV-TR criteria for schizophrenia or schizoaffective disorder were recruited from January 2011 to December 2012 and were randomized to receive either raloxifene 120 mg/d plus antipsychotics or placebo plus antipsychotics...
May 23, 2017: Journal of Clinical Psychiatry
https://www.readbyqxmd.com/read/28529128/role-of-gper-in-estrogen-dependent-nitric-oxide-formation-and-vasodilation
#13
Natalie C Fredette, Matthias R Meyer, Eric R Prossnitz
Estrogens are potent regulators of vasomotor tone, yet underlying receptor- and ligand-specific signaling pathways remain poorly characterized. The primary physiological estrogen 17β-estradiol (E2), a non-selective agonist of classical nuclear estrogen receptors (ERα and ERβ) as well as the G protein-coupled estrogen receptor (GPER), stimulates formation of the vasodilator nitric oxide (NO) in endothelial cells. Here, we studied the contribution of GPER signaling in E2-dependent activation of endothelial NO formation and subsequent vasodilation...
May 18, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28523264/erratum-to-raloxifene-administration-in-women-treated-with-long-term-gonadotropin-releasing-hormone-agonist-for-severe-endometriosis-effects-on-bone-mineral-density
#14
Young Hwa Cho, Mi Jung Um, Suk Jin Kim, Soo Ah Kim, Hyuk Jung
[This corrects the article on p. 174 in vol. 22, PMID: 28119898.].
April 2017: Journal of Menopausal Medicine
https://www.readbyqxmd.com/read/28523260/combination-therapy-of-raloxifene-and-alendronate-for-treatment-of-osteoporosis-in-elderly-women
#15
Mi Jung Um, Eun A Cho, Hyuk Jung
OBJECTIVES: To evaluate and compare the efficacy and safety of the combination of raloxifene and alendronate with those of monotherapies in elderly women with osteoporosis. METHODS: Sixty-two postmenopausal women (mean age 63.5 ± 0.5 years) attending gynecologic osteoporosis clinics with established osteoporosis were randomly allocated to one of four treatment groups and monitored for 3 years. All patients enrolled in this study, including those in the control group (n = 14), received 1...
April 2017: Journal of Menopausal Medicine
https://www.readbyqxmd.com/read/28509316/effects-of-17%C3%AE-estradioland-raloxifene-on-endothelial-opg-and-rankl-secretion
#16
Wojciech Karwowski, Katarzyna Lekesiz, Ewa Koc-Żórawska, Krzysztof Wnuczko, Hanna Borysewicz-Sanczyk, Beata Naumnik
OBJECTIVES: This study aims to asses the effects of estradiol vs. raloxifene on the levels of osteoprotegerin and soluble Receptor Activator of Nuclear Factor kB Ligand (sRANKL) in Human Umbilical Vein Endothelial Cells (HUVEC) culture in standard and calcifying medium. MATERIAL AND METHODS: Human Umbilical Vein Endothelial Cells were isolated from human umbilical vein by standard method. The supernatant concentrations of osteoprotegerin (OPG) and sRANKL (ELISA) were determined after incubation with glicerophosphate, estradiol , raloxifene, glicerophoshate and estradiol, glicerophosphate and raloxifene in comparison with control group at four designated time points (0, 1, 2 and 4 days of incubation)...
2017: Ginekologia Polska
https://www.readbyqxmd.com/read/28492856/treatment-of-low-bone-density-or-osteoporosis-to-prevent-fractures-in-men-and-women-a-clinical-practice-guideline-update-from-the-american-college-of-physicians
#17
Amir Qaseem, Mary Ann Forciea, Robert M McLean, Thomas D Denberg
Description: This guideline updates the 2008 American College of Physicians (ACP) recommendations on treatment of low bone density and osteoporosis to prevent fractures in men and women. This guideline is endorsed by the American Academy of Family Physicians. Methods: The ACP Clinical Guidelines Committee based these recommendations on a systematic review of randomized controlled trials; systematic reviews; large observational studies (for adverse events); and case reports (for rare events) that were published between 2 January 2005 and 3 June 2011...
June 6, 2017: Annals of Internal Medicine
https://www.readbyqxmd.com/read/28489426/preparation-characterization-and-in-vitro-evaluation-of-microemulsion-of-raloxifene-hydrochloride
#18
Shiva Golmohammadzadeh, Nafiseh Farhadian, Amir Biriaee, Faranak Dehghani, Bahman Khameneh
Raloxifene hydrochloride (RLX) is a selective estrogen receptor modulator which is orally used for treatment of osteoporosis and prevention of breast cancer. The drug has low aqueous solubility and bioavailability. The aim of the present study is to formulate and characterize oil-in-water microemulsion systems for oral delivery of RLX. To enhance the drug aqueous solubility, microemulsion based on sesame oil was prepared. Sesame oil and Tween 80 were selected as the drug solvent oil and surfactant, respectively...
May 19, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28449705/large-scale-detection-of-drug-off-targets-hypotheses-for-drug-repurposing-and-understanding-side-effects
#19
Matthieu Chartier, Louis-Philippe Morency, María Inés Zylber, Rafael J Najmanovich
BACKGROUND: Promiscuity in molecular interactions between small-molecules, including drugs, and proteins is widespread. Such unintended interactions can be exploited to suggest drug repurposing possibilities as well as to identify potential molecular mechanisms responsible for observed side-effects. METHODS: We perform a large-scale analysis to detect binding-site molecular interaction field similarities between the binding-sites of the primary target of 400 drugs against a dataset of 14082 cavities within 7895 different proteins representing a non-redundant dataset of all proteins with known structure...
April 28, 2017: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28439061/-calcium-and-bone-metabolism-across-women-s-life-stages-bone-quality-and-treatment-of-osteoporosis-by-serm
#20
Mitsuru Saito, Keishi Marumo
Estrogen deficiency induces bone resorption and bone collagen crosslink abnormalities such as reductions in enzymatic cross-links and accumulation of Advanced glycation end products(AGEs). In this review, we described that the mechanism of poor bone quality in estrogen deficiency and how selective estrogen receptor modulators such as raloxifene and bazedoxifene improve bone structural and material properties.
2017: Clinical Calcium
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