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https://www.readbyqxmd.com/read/28742995/icaritin-induces-mc3t3-e1-subclone14-cell-differentiation-through-estrogen-receptor-mediated-erk1-2-and-p38-signaling-activation
#1
Zhidi Wu, Ling Ou, Chaopeng Wang, Li Yang, Panpan Wang, Hengrui Liu, Yingquan Xiong, Kehuan Sun, Ronghua Zhang, Xiaofeng Zhu
Icaritin (ICT), a hydrolytic product of icariin from the genus Epimedium, has many indicated pharmacological and biological activities. Several studies have shown that ICT has potential osteoprotective effects, including stimulation of osteoblast differentiation and inhibition of osteoclast differentiation. However, the molecular mechanism for this anabolic action of ICT remains largely unknown. Here, we found that ICT could enhance MC3T3-E1 subclone 14 preosteoblastic cell differentiation associated with increased mRNA levels and protein expression of the differentiation markers alkaline phosphatase (ALP), type 1 collagen (COL1), osteocalcin (OC), osteoponin (OPN) and runt-related transcription factor 2 (RUNX2), and improved mineralization, confirmed by bone nodule formation and collagen synthesis...
July 22, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28742842/new-hydrazonoindolin-2-ones-synthesis-exploration-of-the-possible-anti-proliferative-mechanism-of-action-and-encapsulation-into-plga-microspheres
#2
Mohamed I Attia, Wagdy M Eldehna, Samar A Afifi, Adam B Keeton, Gary A Piazza, Hatem A Abdel-Aziz
The synthesis and molecular characterization of new isatin-based hydrazonoindolin-2-ones 4a-o and 7a-e are reported. The in vitro anti-proliferative potential of the synthesized compounds 4a-o and 7a-e was examined against HT-29 (colon), ZR-75 (breast) and A549 (lung) human cancer cell lines. Compounds 7b, 7d and 7e were the most active congeners against the tested human cancer cell lines with average IC50 values of 4.77, 3.39 and 2.37 μM, respectively, as compared with the reference isatin-based drug, sunitinib, which exhibited an average IC50 value of 8...
2017: PloS One
https://www.readbyqxmd.com/read/28742586/summary-of-future-developments
#3
Jessica R Zolton, Alan Decherney
Endometriosis is a chronic disease with the potential to cause devastating clinical manifestations such as infertility and chronic pelvic disease. Current treatment is limited to surgical intervention and pharmacologic therapy targeting estrogen and progesterone to suppress ectopic endometrial tissue proliferation. Undesired side effects and contraindications to the use of hormonal medications may reduce treatment options. As the pathogenesis of endometriosis continues to be investigated, new therapies will emerge...
September 2017: Clinical Obstetrics and Gynecology
https://www.readbyqxmd.com/read/28742547/celiprolol-a-unique-selective-adrenoceptor-modulator
#4
James J Nawarskas, Angela Cheng-Lai, William H Frishman
Celiprolol is a β-blocker with a unique pharmacologic profile: it is a β1-andrenoceptor antagonist with partial β2 agonist activity. Given this combination of effects, celiprolol may be better described as a elective adrenoreceptor modulator. It has antihypertensive and antianginal properties and is indicated for those uses in various countries around the world. In the United States, however, the proposed indication for this drug will be for the treatment of vascular type Ehlers-Danlos syndrome, a rare connective tissue isorder haracterized by fragile arterial structure and an increased risk of life-threatening vascular complications...
July 20, 2017: Cardiology in Review
https://www.readbyqxmd.com/read/28742396/valbenazine-for-tardive-dyskinesia
#5
Oliver Freudenreich, Gary Remington
Tardive dyskinesia (TD) remains a clinical concern for any patient who receives an antipsychotic. While the overall risk of developing TD is lower with newer antipsychotics compared to older agents, a significant number of patients who require long-term treatment will develop TD. Recently, valbenazine (brand name Ingrezza) became the first drug to be approved by the FDA specifically for the treatment of TD. In this New Drug Review, we summarize the basic pharmacology and clinical trial results for valbenazine...
2017: Clinical Schizophrenia & related Psychoses
https://www.readbyqxmd.com/read/28742231/different-resuscitation-strategies-and-novel-pharmacologic-treatment-with-valproic-acid-in-traumatic-brain-injury
#6
REVIEW
Simone E Dekker, Vahagn C Nikolian, Martin Sillesen, Ted Bambakidis, Patrick Schober, Hasan B Alam
Traumatic brain injury (TBI) is a leading cause of death in young adults, and effective treatment strategies have the potential to save many lives. TBI results in coagulopathy, endothelial dysfunction, inflammation, cell death, and impaired epigenetic homeostasis, ultimately leading to morbidity and/or mortality. Commonly used resuscitation fluids such as crystalloids or colloids have several disadvantages and might even be harmful when administered in large quantities. There is a need for next-generation treatment strategies (especially in the prehospital setting) that minimize cellular damage, improve survival, and enhance neurological recovery...
July 25, 2017: Journal of Neuroscience Research
https://www.readbyqxmd.com/read/28742215/complementary-and-alternative-medicine-use-among-us-adults-with-headache-or-migraine-results-from-the-2012-national-health-interview-survey
#7
Yan Zhang, Jeff A Dennis, Matthew J Leach, Felicity L Bishop, Holger Cramer, Vincent C H Chung, Craig Moore, Romy Lauche, Ron Cook, David Sibbritt, Jon Adams
BACKGROUND: Given the safety concerns regarding pharmacological agents, and the considerable impact of headache and migraine on the sufferer's quality of life, many people seek other treatment options beyond conventional medication and care to address their symptoms; this includes complementary and alternative medicine (CAM). Some CAM interventions have shown promising results in clinical trials of headache and migraine management. Nonetheless, there has been little research exploring the reasons for using CAM, and the types of CAM used, among this population...
July 25, 2017: Headache
https://www.readbyqxmd.com/read/28742141/bruton-s-tyrosine-kinase-inhibitor-bms-986142-in-experimental-models-of-rheumatoid-arthritis-enhances-efficacy-of-agents-representing-clinical-standard-of-care
#8
Kathleen M Gillooly, Claudine Pulicicchio, Mark A Pattoli, Lihong Cheng, Stacey Skala, Elizabeth M Heimrich, Kim W McIntyre, Tracy L Taylor, Daniel W Kukral, Shailesh Dudhgaonkar, Jignesh Nagar, Dana Banas, Scott H Watterson, Joseph A Tino, Aberra Fura, James R Burke
Bruton's tyrosine kinase (BTK) regulates critical signal transduction pathways involved in the pathobiology of rheumatoid arthritis (RA) and other autoimmune disorders. BMS-986142 is a potent and highly selective reversible small molecule inhibitor of BTK currently being investigated in clinical trials for the treatment of both RA and primary Sjögren's syndrome. In the present report, we detail the in vitro and in vivo pharmacology of BMS-986142 and show this agent provides potent and selective inhibition of BTK (IC50 = 0...
2017: PloS One
https://www.readbyqxmd.com/read/28742108/fasting-metabolism-modulates-the-interleukin-12-interleukin-10-cytokine-axis
#9
Johannes J Kovarik, Elisabeth Kernbauer, Markus A Hölzl, Johannes Hofer, Guido A Gualdoni, Klaus G Schmetterer, Fitore Miftari, Yury Sobanov, Anastasia Meshcheryakova, Diana Mechtcheriakova, Nadine Witzeneder, Georg Greiner, Anna Ohradanova-Repic, Petra Waidhofer-Söllner, Marcus D Säemann, Thomas Decker, Gerhard J Zlabinger
A crucial role of cell metabolism in immune cell differentiation and function has been recently established. Growing evidence indicates that metabolic processes impact both, innate and adaptive immunity. Since a down-stream integrator of metabolic alterations, mammalian target of rapamycin (mTOR), is responsible for controlling the balance between pro-inflammatory interleukin (IL)-12 and anti-inflammatory IL-10, we investigated the effect of upstream interference using metabolic modulators on the production of pro- and anti-inflammatory cytokines...
2017: PloS One
https://www.readbyqxmd.com/read/28741970/efficacy-and-safety-of-once-weekly-semaglutide-for-the-treatment-of-type-2-diabetes
#10
Xueying Tan, Xiaojing Cao, Minzhi Zhou, Ping Zou, Jingbo Hu
Type 2 diabetes is a chronic metabolic disease characterized by persistent hyperglycemia resulting from progressive deficient of insulin in patients with a background of insulin resistance. Current treatment algorithms recommended by American Diabetes Association/The European Association for the Study of Diabetes promote a patient-centered approach that takes into account a comprehensive consideration of pharmacological properties of drugs, including glucose-lowering action, effects on body weight, correction on multiple pathophysiologic defects, tolerability, and long-term safety...
July 25, 2017: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/28741800/eteplirsen-for-the-treatment-of-duchenne-muscular-dystrophy-quality-of-evidence-concerns-an-alternative-viewpoint
#11
Adriane N Irwin, Megan C Herink
We read the paper by Reinig AM and colleagues entitled "Advances in the Treatment of Duchenne Muscular Dystrophy: New and Emerging Pharmacotherapies" with great interest.(1) The authors discuss several novel therapies to increase production of dystrophin in myocytes, of which, eteplirsen (Exondys) is the only currently approved by the US Food & Drug Administration (FDA).(2) Pharmacologic management of Duchenne muscular dystrophy (DMD) centers on the use of glucocorticoids which works by decreasing inflammation and reducing immune system activity...
July 25, 2017: Pharmacotherapy
https://www.readbyqxmd.com/read/28741230/new-therapeutic-strategies-for-lewy-body-dementias
#12
REVIEW
Latha Velayudhan, Dominic Ffytche, Clive Ballard, Dag Aarsland
This article reviews current treatment strategies and recent advances for the Lewy body dementias (LBDs). Current available symptom treatment strategies are based on monoaminergic, cholinergic and glutaminergic neurotransmitter systems. Relatively robust evidence exists for cholinesterase inhibitors for cognitive impairment in LBD and in Parkinson's disease for antidepressants, clozapine and recently pimavanserin for psychosis. interpidine (RVT 101) and nelotanserin are currently under investigation. Non-pharmacological interventions, such as cognitive stimulation, physical exercises and neuromodulation strategies, may be useful in Parkinson's disease but have not yet been tested in dementias...
September 2017: Current Neurology and Neuroscience Reports
https://www.readbyqxmd.com/read/28741130/epigenetic-involvement-in-etiopathogenesis-and-implications-in-treatment-of-systemic-lupus-erythematous
#13
REVIEW
Arron Munggela Foma, Saeed Aslani, Jafar Karami, Ahmadreza Jamshidi, Mahdi Mahmoudi
BACKGROUND: Recent researches in the field of genetics have extended our knowledge through the discovery of genetic factors associated with autoimmune diseases (AID). Genetics by itself, however, cannot elucidate all the uncertainties encountered in the etiopathology of AID. On the other hand, incomplete harmony in the prevalence of AID in identical twins suggests that non-genetic factors may play an important role in determining the disease susceptibility. Besides, epigenetics, which is defined by changes in gene expression without a corresponding change in the DNA sequences, has come in to provide new awareness in the disease etiopathology by bridging the genetic and epigenetic factors...
July 24, 2017: Inflammation Research: Official Journal of the European Histamine Research Society ... [et Al.]
https://www.readbyqxmd.com/read/28741031/inhibition-of-serotonin-transporters-disrupts-the-enhancement-of-fear-memory-extinction-by-3-4-methylenedioxymethamphetamine-mdma
#14
Matthew B Young, Seth D Norrholm, Lara M Khoury, Tanja Jovanovic, Sheila A M Rauch, Collin M Reiff, Boadie W Dunlop, Barbara O Rothbaum, Leonard L Howell
RATIONALE: 3,4-Methylenedioxymethamphetamine (MDMA) persistently improves symptoms of post-traumatic stress disorder (PTSD) when combined with psychotherapy. Studies in rodents suggest that these effects can be attributed to enhancement of fear memory extinction. Therefore, MDMA may improve the effects of exposure-based therapy for PTSD, particularly in treatment-resistant patients. However, given MDMA's broad pharmacological profile, further investigation is warranted before moving to a complex clinical population...
July 24, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28740732/low-molecular-weight-ngf-mimetic-corrects-the-cognitive-deficit-and-depression-like-behavior-in-experimental-diabetes
#15
R U Ostrovskaya, S S Yagubova, T A Gudasheva, S B Seredenin
Based on the comorbidity of diabetes, depression, and dementia and recognizing that a deficiency of the nerve growth factor (NGF) is involved in all of these kinds of pathologies, we studied the effect of the mimetic of dimeric dipeptide NGF loop 4, GK-2, on a model of streptozotocin-induced type 2 diabetes in C57Bl/6 mice. GK-2 [hexamethylenediamide bis-(N-monosuccinyl-glutamyl-lysine)] was synthesized at the V.V. Zakusov Scientific Research Institute of Pharmacology. The study revealed the ability of GK-2 to ameliorate hyperglycemia induced by streptozotocine (STZ 100 mg/kg i...
April 2017: Acta Naturae
https://www.readbyqxmd.com/read/28740637/antipsychotic-induced-hyperprolactinemia-in-tourette-syndrome
#16
REVIEW
Judith J G Rath, Marlies E J Deen, Hessel van Houten, Sebastiaan F T M de Bruijn, Joop van Gerven, Dick Mul
For many years, Tourette syndrome (TS) was considered to be a rare disorder, but tics and TS are now recognized as fairly common childhood-onset conditions. Children and adolescents with TS are frequently treated with antipsychotics, either as monotherapy or in combination with psychostimulants, melatonin and selective serotonin reuptake inhibitors (SSRIs). Antipsychotics are most often used in schizophrenia and related psychotic disorders, and in these conditions hyperprolactinemia is one of the most common adverse effects associated with antipsychotics, occurring in 40-50% of patients...
July 2017: Therapeutic Advances in Psychopharmacology
https://www.readbyqxmd.com/read/28740584/cardiovascular-disease-in-acromegaly
#17
Morali D Sharma, Anh V Nguyen, Spandana Brown, Richard J Robbins
In patients with acromegaly, chronic excess of growth hormone (GH) and insulin-like growth factor-1 (IGF-1) leads to the development of acromegalic cardiomyopathy. Its main features are biventricular hypertrophy, diastolic dysfunction, and in later stages, systolic dysfunction and congestive heart failure. Surgical and/or pharmacological treatment of acromegaly and control of cardiovascular risk factors help reverse some of these pathophysiologic changes and decrease the high risk of cardiovascular complications...
April 2017: Methodist DeBakey Cardiovascular Journal
https://www.readbyqxmd.com/read/28740414/the-role-of-endoscopic-therapy-in-obesity-management-intragastric-balloons-and-aspiration-therapy
#18
REVIEW
Nitin Kumar, Shelby Sullivan, Christopher C Thompson
Weight management is increasingly incorporating endoscopic bariatric therapy (EBT). As the global burden of obesity and its comorbidities has increased, it is evident that novel therapeutic approaches will be necessary to address the obesity epidemic. EBTs offer greater efficacy than diet and lifestyle modification and lower invasiveness than bariatric surgery. The US Food and Drug Administration has approved two intragastric balloons and aspiration therapy for the treatment of obesity: Apollo Orbera is indicated for the treatment of Class I and Class II obesity, Re Shape Integrated Dual Balloon system is indicated for the same range with a comorbidity, and Aspire Bariatrics AspireAssist is approved for patients with a body mass index of 35-55 kg/m(2)...
2017: Diabetes, Metabolic Syndrome and Obesity: Targets and Therapy
https://www.readbyqxmd.com/read/28740389/methylphenidate-dose-optimization-for-adhd-treatment-review-of-safety-efficacy-and-clinical-necessity
#19
REVIEW
Michael Huss, Praveen Duhan, Preetam Gandhi, Chien-Wei Chen, Carsten Spannhuth, Vinod Kumar
Attention-deficit/hyperactivity disorder (ADHD) is a chronic psychiatric disorder characterized by hyperactivity and/or inattention and is often associated with a substantial impact on psychosocial functioning. Methylphenidate (MPH), a central nervous system stimulant, is commonly used for pharmacological treatment of adults and children with ADHD. Current practice guidelines recommend optimizing MPH dosage to individual patient needs; however, the clinical benefits of individual dose optimization compared with fixed-dose regimens remain unclear...
2017: Neuropsychiatric Disease and Treatment
https://www.readbyqxmd.com/read/28740372/pharmacological-treatment-of-osteoporosis-in-the-oldest-old
#20
REVIEW
A Vandenbroucke, F P Luyten, J Flamaing, E Gielen
The incidence of osteoporotic fractures increases with age. Consequently, the global prevalence of osteoporotic fractures will increase with the aging of the population. In old age, osteoporosis is associated with a substantial burden in terms of morbidity and mortality. Nevertheless, osteoporosis in old age continues to be underdiagnosed and undertreated. This may, at least partly, be explained by the fact that evidence of the antifracture efficacy of osteoporosis treatments comes mainly from randomized controlled trials in postmenopausal women with a mean age of 70-75 years...
2017: Clinical Interventions in Aging
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