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https://www.readbyqxmd.com/read/28323287/experimental-medication-treatment-approaches-for-depression
#1
REVIEW
D F Ionescu, G I Papakostas
Depression is one of the most common psychiatric conditions. Symptoms can lead to significant disability, which result in impairments in overall quality of life. Though there are many approved antidepressant treatments for depression-including selective serotonin reuptake inhibitors, tricyclic antidepressants and monoamine oxidase inhibitors-about a third of patients do not respond to these medications. Therefore, it is imperative for drug discovery to continue towards the development of novel and rapidly acting compounds, especially for patients with treatment-resistant depression...
March 21, 2017: Translational Psychiatry
https://www.readbyqxmd.com/read/28298895/two-phase-modulation-of-formula-see-text-entry-and-cl-formula-see-text-exchanger-in-submandibular-glands-cells-by-dexmedetomidine
#2
Minjeong Ji, Chul-Kyu Park, Jin Woo Lee, Kook Yang Park, Kuk Hui Son, Jeong Hee Hong
Dexmedetomidine (Dex), a highly selective α2-adrenoceptor agonist, attenuates inflammatory responses induced by lipopolysaccharide (LPS) and induces sedative and analgesic effects. Administration of Dex also reduces salivary secretion in human subjects and inhibits osmotic water permeability in rat cortical collecting ducts. However, little is known about the mechanisms underlying the effects of Dex on salivary glands fluid secretion. We demonstrated the α2-adrenoceptor expression in the basolateral membrane of mouse submandibular glands (SMG)...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28288124/c1-neurons-mediate-a-stress-induced-anti-inflammatory-reflex-in-mice
#3
Chikara Abe, Tsuyoshi Inoue, Mabel A Inglis, Kenneth E Viar, Liping Huang, Hong Ye, Diane L Rosin, Ruth L Stornetta, Mark D Okusa, Patrice G Guyenet
C1 neurons, located in the medulla oblongata, mediate adaptive autonomic responses to physical stressors (for example, hypotension, hemorrhage and presence of lipopolysaccharides). We describe here a powerful anti-inflammatory effect of restraint stress, mediated by C1 neurons: protection against renal ischemia-reperfusion injury. Restraint stress or optogenetic C1 neuron (C1) stimulation (10 min) protected mice from ischemia-reperfusion injury (IRI). The protection was reproduced by injecting splenic T cells that had been preincubated with noradrenaline or splenocytes harvested from stressed mice...
March 13, 2017: Nature Neuroscience
https://www.readbyqxmd.com/read/28274151/pharmacophore-based-design-and-discovery-of-meptazinol-carbamates-as-dual-modulators-of-cholinesterase-and-amyloidogenesis
#4
Qiong Xie, Zhaoxi Zheng, Biyun Shao, Wei Fu, Zheng Xia, Wei Li, Jian Sun, Wei Zheng, Weiwei Zhang, Wei Sheng, Qihong Zhang, Hongzhuan Chen, Hao Wang, Zhuibai Qiu
Multifunctional carbamate-type acetylcholinesterase (AChE) inhibitors with anti-amyloidogenic properties like phenserine are potential therapeutic agents for Alzheimer's disease (AD). We reported here the design of new carbamates using pharmacophore model strategy to modulate both cholinesterase and amyloidogenesis. A five-feature pharmacophore model was generated based on 25 carbamate-type training set compounds. (-)-Meptazinol carbamates that superimposed well upon the model were designed and synthesized, which exhibited nanomolar AChE inhibitory potency and good anti-amyloidogenic properties in in vitro test...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28272324/dl0410-ameliorates-memory-and-cognitive-impairments-induced-by-scopolamine-via-increasing-cholinergic-neurotransmission-in-mice
#5
Wenwen Lian, Jiansong Fang, Lvjie Xu, Wei Zhou, De Kang, Wandi Xiong, Hao Jia, Ai-Lin Liu, Guan-Hua Du
Deficiency of the cholinergic system is thought to play a vital role in cognitive impairment of dementia. DL0410 was discovered as a dual inhibitor of acetylcholinesterase (AChE) and butyrylcholinestease (BuChE), with potent efficiency in in-vitro experiments, but its in vivo effect on the cholinergic model has not been evaluated, and its action mechanism has also not been illustrated. In the present study, the capability of DL0410 in ameliorating the amnesia induced by scopolamine was investigated, and its effect on the cholinergic system in the hippocampus and its binding mode in the active site of AChE was also explored...
March 6, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28271317/cholinergic-anti-inflammatory-pathway-does-not-contribute-to-prevention-of-ulcerative-colitis-by-novel-indoline-carbamates
#6
Helena Shifrin, Odelia Mouhadeb, Nathan Gluck, Chen Varol, Marta Weinstock
Indoline carbamates, AN680 and AN917 decrease cytokines, TNF-α and IL-6 in peritoneal macrophages activated by lipopolysaccharide (LPS) and in mouse tissues after LPS injection. They prevent nuclear translocation of nuclear factor κB (NF-κB) and activator protein 1. Only AN917 inhibits cholinesterase (ChE) at relevant concentrations. ChE inhibitors decrease NF-κB by activating α7 nicotinic acetylcholine receptors (α7nAChR). The current study compared the effect of rivastigmine, a ChE inhibitor, AN680 and AN917 on ulcerative colitis induced in mice by ingestion of dextran sodium sulfate (4...
March 7, 2017: Journal of Neuroimmune Pharmacology: the Official Journal of the Society on NeuroImmune Pharmacology
https://www.readbyqxmd.com/read/28260511/clinically-relevant-drug-interactions-with-anti-alzheimer-s-drugs
#7
Filippo Caraci, Janet Sultana, Filippo Drago, Edoardo Spina
The aging world population had led to an increase in the prevalence of Alzheimer's disease (AD). The drugs used to slow down the onset of AD, galantamine, donepezil, rivastigmine and memantine, are generally well-tolerated. However, drug interactions between these drugs and other drugs are an important aspect of patient safety that should be borne in mind, particularly given the high burden of polypharmacy in the elderly. The aim of this review is to provide an updated review of clinically significant drug-drug interactions concerning drugs approved for AD...
March 3, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/28245707/standardized-extract-of-lactuca-sativa-linn-and-its-fractions-abrogates-scopolamine-induced-amnesia-in-mice-a-possible-cholinergic-and-antioxidant-mechanism
#8
Jai Malik, Jagpreet Kaur, Sunayna Choudhary
OBJECTIVES: The present study was designed to evaluate the efficacy of Lactuca sativa (LS) Linn. (Asteraceae) against scopolamine- induced amnesia and to validate its traditional claim as memory enhancer. METHODS: Ethanol extract of fresh LS leaves (LSEE), standardized on the basis of quercetin content, was successively partitioned using various solvents viz., hexane, ethyl acetate, and n-butanol in increasing order of polarity. LSEE (50, 100, and 200 mg/kg) and its various fractions (at a dose equivalent to dose of LSEE exhibiting maximum activity), administered orally for 14 days, were evaluated for their memory enhancing effect against scopolamine-induced (1 mg/kg, i...
February 28, 2017: Nutritional Neuroscience
https://www.readbyqxmd.com/read/28228069/recent-advances-in-the-gastric-mucosal-protection-against-stress-induced-gastric-lesions-importance-of-renin-angiotensin-vasoactive-metabolites-gaseous-mediators-and-appetite-peptides
#9
Tomasz Brzozowski, Katarzyna Magierowska, Marcin Magierowski, Agata Ptak-Belowska, Robert Pajdo, Slawomir Kwiecien, Rafal Olszanecki, Ryszard Korbut
Stress is known to cause severe adverse effects in the human gastrointestinal tract including mucosal microbleedings and erosions or even gastric ulceration but the mechanism of these complications has not been fully elucidated. The pathogenesis of stress-induced gastric damage involves the fall in gastric blood flow (GBF), an increase in gastric acid secretion and gastric motility, enhanced adrenergic and cholinergic nerve activity and the rise in gastric mucosal generation of reactive oxygen species. The gastric mucosal defense mechanisms against the deleterious effect of stress include the activation of the hypothalamic-pituitary-adrenal axis which has been linked with glucocorticoids release capable of counteracting of stress-induced gastric lesions...
February 20, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28224377/curcumin-attenuates-surgery-induced-cognitive-dysfunction-in-aged-mice
#10
Xiang Wu, Huixin Chen, Chunhui Huang, Xinmei Gu, Jialing Wang, Dilin Xu, Xin Yu, Chu Shuai, Liping Chen, Shun Li, Yiguo Xu, Tao Gao, Mingrui Ye, Wei Su, Haixiong Liu, Jinrong Zhang, Chuang Wang, Junping Chen, Qinwen Wang, Wei Cui
Post-operative cognitive dysfunction (POCD) is associated with elderly patients undergoing surgery. However, pharmacological treatments for POCD are limited. In this study, we found that curcumin, an active compound derived from Curcuma longa, ameliorated the cognitive dysfunction following abdominal surgery in aged mice. Further, curcumin prevented surgery-induced anti-oxidant enzyme activity. Curcumin also increased brain-derived neurotrophic factor (BDNF)-positive area and expression of pAkt in the brain, suggesting that curcumin activated BDNF signaling in aged mice...
February 21, 2017: Metabolic Brain Disease
https://www.readbyqxmd.com/read/28209997/antisense-mir-132-blockade-via-the-ache-r-splice-variant-mitigates-cortical-inflammation
#11
Nibha Mishra, Lyndon Friedson, Geula Hanin, Uriya Bekenstein, Meshi Volovich, Estelle R Bennett, David S Greenberg, Hermona Soreq
MicroRNA (miR)-132 brain-to-body messages suppress inflammation by targeting acetylcholinesterase (AChE), but the target specificity of 3'-AChE splice variants and the signaling pathways involved remain unknown. Using surface plasmon resonance (SPR), we identified preferential miR-132 targeting of soluble AChE-R over synaptic-bound AChE-S, potentiating miR-132-mediated brain and body cholinergic suppression of pro-inflammatory cytokines. Inversely, bacterial lipopolysaccharide (LPS) reduced multiple miR-132 targets, suppressed AChE-S more than AChE-R and elevated inflammatory hallmarks...
February 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28197102/right-cervical-vagotomy-aggravates-viral-myocarditis-in-mice-via-the-cholinergic-anti-inflammatory-pathway
#12
Ge Li-Sha, Chen Xing-Xing, Wu Lian-Pin, Zhou De-Pu, Li Xiao-Wei, Lin Jia-Feng, Li Yue-Chun
The autonomic nervous system dysfunction with increased sympathetic activity and withdrawal of vagal activity may play an important role in the pathogenesis of viral myocarditis. The vagus nerve can modulate the immune response and control inflammation through a 'cholinergic anti-inflammatory pathway' dependent on the α7-nicotinic acetylcholine receptor (α7nAChR). Although the role of β-adrenergic stimulation on viral myocarditis has been investigated in our pervious studies, the direct effect of vagal tone in this setting has not been yet studied...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28192749/ascorbic-acid-ameliorates-behavioural-deficits-and-neuropathological-alterations-in-rat-model-of-alzheimer-s-disease
#13
Olayemi Joseph Olajide, Emmanuel Olusola Yawson, Ismail Temitayo Gbadamosi, Tolulope Timothy Arogundade, Ezra Lambe, Kosisochukwu Obasi, Ismail Tayo Lawal, Abdulmumin Ibrahim, Kehinde Yomi Ogunrinola
Exploring the links between neural pathobiology and behavioural deficits in Alzheimer's disease (AD), and investigating substances with known therapeutic advantages over subcellular mechanisms underlying these dysfunctions could advance the development of potent therapeutic molecules for AD treatment. Here we investigated the efficacy of ascorbic acid (AA) in reversing aluminium chloride (AlCl3)-induced behavioural deficits and neurotoxic cascades within prefrontal cortex (PFC) and hippocampus of rats. A group of rats administered oral AlCl3 (100mg/kg) daily for 15days showed degenerative changes characterised by significant weight loss, reduced exploratory/working memory, frontal-dependent motor deficits, cognitive decline, memory dysfunction and anxiety during behavioural assessments compared to control...
March 2017: Environmental Toxicology and Pharmacology
https://www.readbyqxmd.com/read/28178923/non-neuronal-cholinergic-activity-is-potentiated-in-myasthenia-gravis
#14
Bin Han, Chao Zhang, Shoufeng Liu, Yiping Xia, Hao Sun, Zhongying Gong, Alain R Simard, Qiang Liu, Junwei Hao
BACKGROUND: Non-neuronal acetylcholine (ACh) restricts autoimmune responses and attenuates inflammation by cholinergic anti-inflammation pathway. To date, the implication of ACh in myasthenia gravis (MG) remained unexplored. This study aimed to investigate the possible relationship between ACh levels, anti-muscle-specific tyrosine kinase (MuSK) antibody titers, main clinical features and outcomes of MG patients. METHODS: We successfully measured ACh levels in human peripheral blood mononuclear cells (PBMCs) from 125 MG patients and 50 matched healthy controls by using ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS)...
February 8, 2017: BMC Neurology
https://www.readbyqxmd.com/read/28174611/pterostilbene-ameliorates-intracerebroventricular-streptozotocin-induced-memory-decline-in-rats
#15
Bhagyashree Naik, Abhijit Nirwane, Anuradha Majumdar
There is strong evidence that mitochondrial dysfunction mediated oxidative stress results in aging and energy metabolism deficits thus playing a prime role in pathogenesis of Alzheimer's disease, neuronal death and cognitive dysfunction. Evidences accrued in empirical studies suggest the antioxidant, anticancer and anti-inflammatory activities of the phytochemical pterostilbene (PTS). PTS also exhibits favourable pharmacokinetic attributes compared to other stilbenes. Hence, in the present study, we explored the neuroprotective role of PTS in ameliorating the intracerebroventricular administered streptozotocin (STZ) induced memory decline in rats...
February 2017: Cognitive Neurodynamics
https://www.readbyqxmd.com/read/28168765/prediction-of-anti-alzheimer-s-activity-of-flavonoids-targeting-acetylcholinesterase-in-silico
#16
Subrata Das, Monjur A Laskar, Satyajit D Sarker, Manabendra D Choudhury, Prakash Roy Choudhury, Abhijit Mitra, Shajarahtunnur Jamil, Siti Mariam A Lathiff, Siti Awanis Abdullah, Norazah Basar, Lutfun Nahar, Anupam D Talukdar
INTRODUCTION: Prenylated and pyrano-flavonoids of the genus Artocarpus J. R. Forster & G. Forster are well known for their acetylcholinesterase (AChE) inhibitory, anti-cholinergic, anti-inflammatory, anti-microbial, anti-oxidant, anti-proliferative and tyrosinase inhibitory activities. Some of these compounds have also been shown to be effective against Alzheimer's disease. OBJECTIVE: The aim of the in silico study was to establish protocols to predict the most effective flavonoid from prenylated and pyrano-flavonoid classes for AChE inhibition linking to the potential treatment of Alzheimer's disease...
February 7, 2017: Phytochemical Analysis: PCA
https://www.readbyqxmd.com/read/28167290/albizia-zygia-dc-j-f-macbr-leguminosae-mimosoideae-root-extract-exhibits-anti-nociceptive-and-antipyretic-activities-in-murine-models
#17
Wonder Kofi Mensah Abotsi, Stanley Benjamin Lamptey, Eric Boakye-Gyasi, Eric Woode
ETHNOPHARMACOLOGICAL RELEVANCE: The root extract of Albizia zygia (DC.) J.F. Macbr. (Leguminosae-Mimosoideae) is traditionally used in the management of pain and fever. However, little scientific data exists in literature to support its use. AIM OF STUDY: The present study evaluated the anti-nociceptive and antipyretic properties of the hydroethanolic extract of the roots of Albizia zygia in animal models. MATERIALS AND METHODS: The analgesic effects were investigated in chemical (acetic acid-induced abdominal writhing and formalin tests), thermal (tail-immersion test) and mechanical (carrageenan-induced hyperalgesia) pain models...
February 3, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28156664/association-between-anti-cholinergic-burden-and-delirium-among-patients-with-advanced-cancer-referred-to-a-palliative-care-consult-service
#18
Joseph Baidoo, Vishidha Reddy Balankari, Jessica Marie Waletich-Flemming, Marvin Delgado-Guay, Jimin Wu, Diane D Liu, Eduardo Bruera
213 Background: Delirium occurs in about 45-60% hospitalized patients and 80-85% at the end of life. Predisposing factors include anti-cholinergic medications as is often cited in the geriatric literature. Our study aimed to demonstrate the association of anti-cholinergic burden and delirium in patients with advanced cancer. METHODS: Retrospective review of 775 consecutive patients seen by the palliative care inpatient consult team. Demographic data, MDAS, ECOG, and anti-cholinergic drugs were determined...
October 9, 2016: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/28155595/cholinergic-anti-inflammatory-pathway-and-stroke
#19
Kamil Duris, Jolana Lipkova, Michal Jurajda
Stroke is devastating cerebrovascular event which is responsible for 6.7 million deaths each year worldwide. Inflammation plays an important role in the pathophysiology of stroke. Targeting inflammation after stroke is highly actual topic for both experimental and clinical research. Cholinergic anti-inflammatory pathway (CHAIP) is a physiological mechanism by which central nervous system regulates immune response and controls inflammation. Vagus nerve, spleen and α7 nicotinic acetylcholine receptor (α7 nAChR) are the main components of CHAIP...
February 1, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28152649/anti-inflammatory-anti-cholinergic-and-cytotoxic-effects-of-sida-rhombifolia
#20
Siau Hui Mah, Soek Sin Teh, Gwendoline Cheng Lian Ee
CONTEXT: Sida (Malvaceae) has been used as a traditional remedy for the treatment of diarrhoea, malarial, gastrointestinal dysentery, fevers, asthma and inflammation. OBJECTIVES: This study evaluates the anti-inflammatory, cytotoxic and anti-cholinergic activities of Sida rhombifolia Linn. whole plant for the first time. MATERIALS AND METHODS: S. rhombifolia whole plant was extracted by n-hexane, ethyl acetate and methanol using Soxhlet apparatus...
December 2017: Pharmaceutical Biology
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