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https://www.readbyqxmd.com/read/29677630/resting-heart-rate-and-the-incidence-and-progression-of-valvular-calcium-the-multi-ethnic-study-of-atherosclerosis-mesa
#1
Kojo Amoakwa, Oluwaseun E Fashanu, Martin Tibuakuu, Di Zhao, Eliseo Guallar, Seamus P Whelton, Wesley T O'Neal, Wendy S Post, Matthew J Budoff, Erin D Michos
BACKGROUND AND AIMS: Left-sided valvular calcification is associated with cardiovascular disease (CVD) morbidity and mortality. Resting heart rate (RHR) may influence valvular calcium progression through shear stress. Whether RHR, an established CVD risk factor, is associated with valvular calcium progression is unknown. We assessed whether RHR predicts incidence and progression of mitral annular calcium (MAC) and aortic valve calcium (AVC) in a community-based cohort free of CVD at baseline...
April 6, 2018: Atherosclerosis
https://www.readbyqxmd.com/read/29677540/ameliorating-effect-of-berbamine-on-hepatic-key-enzymes-of-carbohydrate-metabolism-in-high-fat-diet-and-streptozotocin-induced-type-2-diabetic-rats
#2
Sankaranarayanan Chandrasekaran, Nishanthi Ramajayam, Pugalendi Pachaiappan
BACKGROUND: Aberrations in the activities of key enzymes of carbohydrate metabolism is well documented in diabetes mellitus. Previous studies have shown that active ingredients in the extracts of Berberis aristata exhibits diverse pharmacological activities in animal models. OBJECTIVE: The present study was undertaken to investigate whether berbamine (BBM), an alkaloid from the roots of Berberis aristata can ameliorate the altered activities of carbohydrate metabolic enzymes in high fat diet (HFD)/streptozotocin (STZ) induced diabetic rats...
April 17, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29677442/synthesis-and-pharmacological-evaluation-of-novel-c-8-substituted-tetrahydroquinolines-as-balanced-affinity-mu-delta-opioid-ligands-for-the-treatment-of-pain
#3
Anthony F Nastase, Nicholas W Griggs, Jessica P Anand, Thomas J Fernandez, Aubrie A Harland, Tyler J Trask, Emily M Jutkiewicz, John R Traynor, Henry I Mosberg
The use of opioids for the treatment of pain, while largely effective, is limited by detrimental side effects including analgesic tolerance, physical dependence, and euphoria, which may lead to opioid abuse. Studies have shown that compounds with a -opioid receptor (MOR) agonist/-opioid receptor (DOR) antagonist profile reduce or eliminate some of these side effects including development of tolerance and dependence. Herein we report the synthesis and pharmacological evaluation of a series of tetrahydroquinoline-based peptidomimetics with substitutions at the C-8 position...
April 20, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29677175/are-antipsychotics-effective-for-the-prevention-of-postoperative-delirium
#4
Viviana Castro, Rami Guinguis, Marcela Carrasco
INTRODUCTION: Antipsychotics have been proposed as a pharmacological alternative to prevent postoperative delirium. Nonetheless, their actual clinical benefits and harms are a matter of debate. METHODS: To answer this question, we used Epistemonikos, the largest database of systematic reviews in health, which is maintained by screening multiple information sources, including MEDLINE, EMBASE, Cochrane, among others. We extracted data from the chosen systematic reviews, reanalyzed the data from the primary studies, conducted a meta-analysis and generated a summary of findings table using the GRADE approach...
April 20, 2018: Medwave
https://www.readbyqxmd.com/read/29677122/applications-of-the-fiv-model-to-study-hiv-pathogenesis
#5
REVIEW
Craig Miller, Zaid Abdo, Aaron Ericsson, John Elder, Sue VandeWoude
Feline immunodeficiency virus (FIV) is a naturally-occurring retrovirus that infects domestic and non-domestic feline species, producing progressive immune depletion that results in an acquired immunodeficiency syndrome (AIDS). Much has been learned about FIV since it was first described in 1987, particularly in regard to its application as a model to study the closely related lentivirus, human immunodeficiency virus (HIV). In particular, FIV and HIV share remarkable structure and sequence organization, utilize parallel modes of receptor-mediated entry, and result in a similar spectrum of immunodeficiency-related diseases due to analogous modes of immune dysfunction...
April 20, 2018: Viruses
https://www.readbyqxmd.com/read/29677028/treatment-of-tobacco-dependence-current-state-of-the-art
#6
Hasmeena Kathuria, Frank T Leone, Enid R Neptune
PURPOSE OF REVIEW: The Centers for Medicare and Medicaid Services' requirement to integrate tobacco treatment with lung cancer screening (LCS) has served as a catalyst for motivating pulmonary medicine clinicians to improve upon their ability to effectively treat tobacco dependence. To do so, clinicians need to be well versed in the behavioral and pharmacologic tools that promote smoking cessation. RECENT FINDINGS: The current review outlines current strategies for treating tobacco dependence, focusing on the important interplay between counseling and pharmacotherapy...
April 18, 2018: Current Opinion in Pulmonary Medicine
https://www.readbyqxmd.com/read/29676941/pk-pd-evaluation-of-fimasartan-for-the-treatment-of-hypertension-current-evidences-and-future-perspectives
#7
Fabio Angeli, Paolo Verdecchia, Monica Trapasso, Marina Pane, Sara Signorotti, Gianpaolo Reboldi
Fimasartan is the ninth and latest Angiotensin Receptor Blockers for the treatment of hypertension. Fimasartan is a derivative of losartan in which the imidazole ring has been replaced, a change that provided higher potency and longer duration than losartan. It provides a selective type 1 angiotensin II receptor antagonist effect with noncompetitive, insurmountable binding. Fimasartan is rapidly absorbed following oral administration with an oral bioavailability of 18.6 ± 7.2 %. Fimasartan is relatively stable in terms of metabolism and more than 90 % of circulating fimasartan moieties in the plasma are in the parent form; fecal elimination and biliary excretion are the predominant elimination pathways of fimasartan...
April 20, 2018: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/29676829/er-stress-mediated-autophagy-protects-against-%C3%AE-%C3%AE-dimethylacrylshikonin-induced-apoptosis-in-lung-adenocarcinoma-cells
#8
Haibing Wang, Gaochenxi Zhang
β,β-Dimethylacrylshikonin (DMAS) is an anti-cancer compound extracted from the roots of Lithospermum erythrorhizon. This study aims to investigate the effects of DMAS on human lung adenocarcinoma cells in vitro and explored the mechanisms of its anti-cancer action. We demonstrated that DMAS markedly inhibited cell viability in a dose- and time-dependent manner, and induced apoptosis as well as autophagy in human lung adenocarcinoma cells. Furthermore, we found that DMAS stimulated endoplasmic reticulum (ER) stress and mediated autophagy via the PERK-eIF2α-ATF4-CHOP and IRE1-TRAF2-JNK axises of the unfolded protein response (UPR) in human lung adenocarcinoma cells...
April 20, 2018: Cancer Science
https://www.readbyqxmd.com/read/29676239/transdermal-delivery-of-at1-receptor-antagonists-reduce-blood-pressure-and-reveals-a-vasodilatory-effect-in-kidney-blood-vessels
#9
Vasso Apostolopoulos, Michaila Michalatou, Maria-Eleni Androutsou, Markos Antonopoulos, George Agelis, Anthony Zulli, Tawar Qaradakhi, John Matsoukas
BACKGROUND: The Renin Angiotensin System (RAS) is pharmacologically targeted to reduce blood pressure, and patient compliance to oral medications is a clinical issue. The mechanisms of action of angiotensin receptor blockers (ARBs) in reducing blood pressure are not well understood, and is purported to be via a reduction of angiotensin II signaling. OBJECTIVE: We aimed to develop a transdermal delivery method for ARBs (losartan potassium and valsartan) and to determine if ARBs reveal a vasodilatory effect of the novel RAS peptide, alamandine...
April 19, 2018: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/29676232/pharmacoepigenetics-and-pharmacoepigenomics-an-overview
#10
Jacob Peedicayil
The rapid and major advances being made in epigenetics is impacting pharmacology, giving rise to new sub-disciplines in pharmacology, pharmacoepigenetics, the study of the epigenetic basis of variation in response to drugs; and pharmacoepigenomics, the application of pharmacoepigenetics on a genome-wide scale. This article gives an overview of the current state of knowledge of pharmacoepigenetics and pharmacoepigenomics. The article highlights the following areas: epigenetic therapy, the role of epigenetics in pharmacokinetics, the relevance of epigenetics to adverse drug reactions, personalized medicine, drug addiction, and drug resistance, and the use of epigenetic biomarkers in drug therapy...
April 19, 2018: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/29676230/insights-into-the-molecular-aspects-of-neuroprotective-bacoside-a-and-bacopaside-i
#11
Vini C Sekhar, Gayathri Viswanathan, Sabulal Baby
Bacopa monnieri, commonly known as Brahmi, has been extensively used as a neuromedicine for various disorders such as anxiety, depression and memory loss. Chemical characterization studies revealed the major active constituents of the herb as the triterpenoid saponins, bacosides. Bacoside A, the vital neuroprotective constituent, is composed of four constituents viz., bacoside A3, bacopaside II, jujubogenin isomer of bacopasaponin C (bacopaside X) and bacopasaponin C. B. monnieri extracts as well as bacosides successfully establish a healthy antioxidant environment in various tissues especially in liver and brain...
April 19, 2018: Current Neuropharmacology
https://www.readbyqxmd.com/read/29676170/discovery-of-novel-dual-acetylcholinesterase-inhibitors-with-antifibrillogenic-activity-related-to-alzheimer-s-disease
#12
Jonathan R de Almeida, Micheli Figueiro, Wanda Pereira Almeida, Carlos Henrique Tomich de Paula da Silva
AIM: Alzheimer's disease is a progressive and neurodegenerative disorder of the CNS, affecting elderly people. The current pharmacological approach is based on the improvement of cholinergic neurotransmission by inhibiting acetylcholinesterase (AChE) with AChE inhibitors. The disease is also characterized by the accelerated accumulation of β-amyloid plaques around neurons. Furthermore, in vitro studies revealed that AChE can induce β-amyloid peptide (Aβ) aggregation. METHODOLOGY: Computer-aided molecular design by virtual screening was here employed to discover novel potential AChE inhibitors, with antifibrillogenic properties, in other words, inhibiting Aβ aggregation...
April 20, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29676114/-pharmacological-effect-of-combined-administration-of-natures-tastes-and-components-of-chinese-herbal-compounds
#13
REVIEW
Chun-Yan Lv, Shao-Wa Lv, Guo-Yu Li, Hai-Xue Kuang
The combined administration of traditional Chinese medicine (TCM) aims at comprehensive adjustment of body based on the theory of TCM and the theory of Chinese medicine property. The natures and tastes of TCM are the core of the theory of TCM property. The combined administration of natures and tastes of TCM is one of the important theories of prescription compatibility. The objective of study on the combined administration of natures and tastes of prescriptions according to symptoms of disease is to clarify the compatibility mechanism of prescriptions...
March 2018: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29676112/-effect-of-animal-medicines-for-extinguishing-wind-to-arrest-convulsions-on-central-nervous-system-diseases
#14
REVIEW
Zhi-Jie Yu, Jin-Song Li, Wei Peng, Ping Wang, Liang Xiong, Yu-Jie Liu, Ying Xu, Tao Sun
The human health is seriously affected by central nervous system(CNS) diseases, but the pathogenesis of CNS diseases is still not completely clear. Currently, the drugs used to treat CNS diseases are mainly receptor modulators and neurotransmitter inhibitors, which have serious side effects; and there are short of drugs for treating CNS diseases clinically. Studies suggest that animal medicines mainly include protein, polypeptide and small-molecule compounds, and have such pharmacological effects in calming, resisting convulsions and improving brain tissues...
March 2018: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29675956/clonidine-modulates-the-activity-of-the-subthalamic-supplementary-motor-loop-evidence-from-a-pharmacological-study-combining-dbs-and-eeg-recordings-in-parkinsonian-patients
#15
Charlotte Spay, Marion Albares, Guillaume Lio, Stephane Thobois, Emmanuel Broussolle, Brian Lau, Benedicte Ballanger, Philippe Boulinguez
Clonidine is an anti-hypertensive medication which acts as an alpha-adrenergic receptors agonist. As the noradrenergic system is likely to support cognitive functions including attention and executive control, other clinical uses of clonidine have recently gained popularity for the treatment of neuropsychiatric disorders like attention-deficit hyperactivity disorder or Tourette syndrome, but the mechanism of action is still unclear. Here, we test the hypothesis that the noradrenergic system regulates the activity of subthalamo-motor cortical loops, and that this influence can be modulated by clonidine...
April 20, 2018: Journal of Neurochemistry
https://www.readbyqxmd.com/read/29675872/identification-and-quantification-of-blood-brain-barrier-transporters-in-isolated-rat-brain-microvessels
#16
Hajar Al Feteisi, Zubida M Al-Majdoub, Brahim Achour, Narciso Couto, Amin Rostami-Hodjegan, Jill Barber
The blood-brain barrier (BBB) maintains brain homeostasis by tightly regulating the exchange of molecules with systemic circulation. It consists primarily of microvascular endothelial cells surrounded by astrocytic endfeet, pericytes, and microglia. Understanding the make-up of transporters in rat BBB is essential to the translation of pharmacological and toxicological observations into humans. In this study, experimental workflows are presented in which the optimization of (a) isolation of rat brain microvessels, (b) enrichment of endothelial cells, and (c) extraction and digestion of proteins were evaluated, followed by identification and quantification of BBB proteins...
April 20, 2018: Journal of Neurochemistry
https://www.readbyqxmd.com/read/29675639/pharmacokinetic-pharmacodynamic-modeling-in-pediatric-drug-development-and-the-importance-of-standardized-scaling-of-clearance
#17
REVIEW
Eva Germovsek, Charlotte I S Barker, Mike Sharland, Joseph F Standing
Pharmacokinetic/pharmacodynamic (PKPD) modeling is important in the design and conduct of clinical pharmacology research in children. During drug development, PKPD modeling and simulation should underpin rational trial design and facilitate extrapolation to investigate efficacy and safety. The application of PKPD modeling to optimize dosing recommendations and therapeutic drug monitoring is also increasing, and PKPD model-based dose individualization will become a core feature of personalized medicine. Following extensive progress on pediatric PK modeling, a greater emphasis now needs to be placed on PD modeling to understand age-related changes in drug effects...
April 19, 2018: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/29675448/intestinal-farnesoid-x-receptor-activation-by-pharmacologic-inhibition-of-the-organic-solute-transporter-%C3%AE-%C3%AE
#18
Sandra M W van de Wiel, D Rudi de Waart, Ronald P J Oude Elferink, Stan F J van de Graaf
Background & Aims: The organic solute transporter α-β (OSTα-OSTβ) mainly facilitates transport of bile acids across the basolateral membrane of ileal enterocytes. Therefore, inhibition of OSTα-OSTβ might have similar beneficial metabolic effects as intestine-specific agonists of the major nuclear receptor for bile acids, the farnesoid X receptor (FXR). However, no OSTα-OSTβ inhibitors have yet been identified. Methods: Here, we developed a screen to identify specific inhibitors of OSTα-OSTβ using a genetically encoded Förster Resonance Energy Transfer (FRET)-bile acid sensor that enables rapid visualization of bile acid efflux in living cells...
March 2018: Cellular and Molecular Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/29675280/what-can-happen-when-postpartum-anxiety-progresses-to-psychosis-a-case-study
#19
Vesna Pirec
This case report describes a primipara without documented psychiatric history prior to complicated delivery. Onset of severe insomnia and anxiety was right after childbirth but not treated. Obsessive thinking pattern became more prominent. The patient became depressed and sought psychiatric help four months after delivery. Insomnia was then treated pharmacologically. Anxiety and depression persisted, suicidal ideation emerged, and the patient became confused, indecisive, overwhelmed, and delusional regarding her child's health...
2018: Case Reports in Psychiatry
https://www.readbyqxmd.com/read/29675269/translation-of-remote-control-regenerative-technologies-for-bone-repair
#20
Hareklea Markides, Jane S McLaren, Neil D Telling, Noura Alom, E'atelaf A Al-Mutheffer, Richard O C Oreffo, Andrew Zannettino, Brigitte E Scammell, Lisa J White, Alicia J El Haj
The role of biomechanical stimuli, or mechanotransduction, in normal bone homeostasis and repair is understood to facilitate effective osteogenesis of mesenchymal stem cells (MSCs) in vitro. Mechanotransduction has been integrated into a multitude of in vitro bone tissue engineering strategies and provides an effective means of controlling cell behaviour towards therapeutic outcomes. However, the delivery of mechanical stimuli to exogenous MSC populations, post implantation, poses a significant translational hurdle...
2018: NPJ Regenerative Medicine
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