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https://www.readbyqxmd.com/read/29614315/a-novel-pharmacological-activity-of-caffeine-in-the-cholinergic-system
#1
Camila Fabiani, Ana Paula Murray, Jeremías Corradi, Silvia Susana Antollini
Cholinergic deficit is regarded as an important factor responsible for Alzheimer's disease (AD) symptoms. Acetylcholinesterase (AChE) and nicotinic receptor (AChR) are two molecular targets for the treatment of this disease. We found here that methanolic extracts of Camellia sinensis exhibited anticholinesterase activity and induced AChR conformational changes. From bioguided fractionation we confirmed that caffeine was the active compound exerting such effects. It is well-known that caffeine acts as an inhibitor of AChE and here we explored the effect of caffeine on the AChR by combining single channel recordings and fluorescent measurements...
March 31, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29521210/phosphodiesterase-10-inhibitors-novel-perspectives-for-psychiatric-and-neurodegenerative-drug-discovery
#2
Agnieszka Zagorska, Anna Partyka, Adam Bucki, Alicja Gawalska, Anna Czopek, Maciej Pawlowski
BACKGROUND: The phosphodiesterase 10 (PDE10) family, identified in 1999, is mainly expressed in the brain, particularly in the striatum, within the medium spiny neurons, nucleus accumbens, and olfactory tubercle. Inhibitors of PDE10 (PDE10-Is) are a conceptually rational subject for medicinal chemistry with potential use in the treatment of psychiatric and neurodegenerative diseases. OBJECTIVE: This review is based on peer-reviewed published articles, and summarizes the cellular and molecular biology of PDE10 as a rational target for psychiatric and neurodegenerative drug discovery...
March 8, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29504423/-caffeine-traditional-and-new-therapeutic-indications-and-use-as-a-dermatological-model-drug
#3
Luca Bors, Ágnes Bajza, Dorottya Kocsis, Franciska Erdő
Coffee consumption had already been described in the 15th century. The spreading of coffee drinking was not only a consequence of its delicious aromatic taste, but also of its pharmacological effects, especially due to its caffeine content. In this review, the mechanisms behind its complex stimulatory effects and the latest studies on the possible new therapeutic indications of caffeine are summarized. Several papers reported the neuroprotective (in Alzheimer's and Parkinson's disease) and hepatoprotective profiles of caffeine, and we show the most promising new results about its preventive properties in dermal malignancies...
March 2018: Orvosi Hetilap
https://www.readbyqxmd.com/read/29497377/long-term-treatment-with-low-dose-caffeine-worsens-bpsd-like-profile-in-3xtg-ad-mice-model-of-alzheimer-s-disease-and-affects-mice-with-normal-aging
#4
Raquel Baeta-Corral, Björn Johansson, Lydia Giménez-Llort
Coffee or caffeine has recently been suggested as prophylaxis for dementia. Although memory problems are hallmarks of Alzheimer's disease, this dementia is also characterized by neuropsychiatric symptoms called Behavioral and Psychological Symptoms of Dementia (BPSD). The impact of preventive/therapeutic strategies on both cognitive and non-cognitive symptoms can be addressed in the 3xTg-AD mice, since they exhibit cognitive but also BPSD-like profiles. Here, we studied the long-term effects of a low dose of caffeine in male 3xTg-AD mice and as compared to age-matched non-transgenic (NTg) counterparts with normal aging...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29495349/neuroprotective-effects-and-mechanisms-of-tea-bioactive-components-in-neurodegenerative-diseases
#5
REVIEW
Shu-Qing Chen, Ze-Shi Wang, Yi-Xiao Ma, Wei Zhang, Jian-Liang Lu, Yue-Rong Liang, Xin-Qiang Zheng
As the population ages, neurodegenerative diseases such as Parkinson's disease (PD) and Alzheimer's disease (AD) impose a heavy burden on society and families. The pathogeneses of PD and AD are complex. There are no radical cures for the diseases, and existing therapeutic agents for PD and AD have diverse side effects. Tea contains many bioactive components such as polyphenols, theanine, caffeine, and theaflavins. Some investigations of epidemiology have demonstrated that drinking tea can decrease the risk of PD and AD...
February 25, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29417473/impact-of-coffee-and-cacao-purine-metabolites-on-neuroplasticity-and-neurodegenerative-disease
#6
Simonetta Camandola, Natalie Plick, Mark P Mattson
Increasing evidence suggests that regular consumption of coffee, tea and dark chocolate (cacao) can promote brain health and may reduce the risk of age-related neurodegenerative disorders. However, the complex array of phytochemicals in coffee and cacao beans and tea leaves has hindered a clear understanding of the component(s) that affect neuronal plasticity and resilience. One class of phytochemicals present in relatively high amounts in coffee, tea and cacao are methylxanthines. Among such methylxanthines, caffeine has been the most widely studied and has clear effects on neuronal network activity, promotes sustained cognitive performance and can protect neurons against dysfunction and death in animal models of stroke, Alzheimer's disease and Parkinson's disease...
February 8, 2018: Neurochemical Research
https://www.readbyqxmd.com/read/28990513/protective-effects-of-the-caffeine-against-neurodegenerative-diseases
#7
Ester Tellone, Antonio Galtieri, Annamaria Russo, Silvana Ficarra
Caffeine is one of the most consumed stimulant of the central nervous system. Similar to those of other stimulants, its effects are to improve brain activity and stimulate cognition learning and memory. Caffeine affects the brain by acting mainly as a non-selective blocker of the adenosine receptors (A1, A2A, A2B, and A3). The purpose of this review article is to provide an overview on the neurobiochemical impact of caffeine, focusing on the ability of the drug to effectively counteract several neurodegenerative disorders such as Alzheimer's, Parkinson's, Huntington's diseases, Multiple sclerosis and Amyotrophic lateral sclerosis and Epilepsy...
October 9, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28895043/effects-of-long-term-caffeine-consumption-on-the-adenosine-a1-receptor-in-the-rat-brain-an-in-vivo-pet-study-with-18-f-cpfpx
#8
Danje Nabbi-Schroeter, David Elmenhorst, Angela Oskamp, Stefanie Laskowski, Andreas Bauer, Tina Kroll
PURPOSE: Caffeine, a nonselective antagonist of adenosine receptors, is the most popular psychostimulant worldwide. Recently, a protective role of moderate chronic caffeine consumption against neurodegenerative diseases such as Alzheimer's and Parkinson's disease has been discussed. Thus, aim of the present study was an in vivo investigation of effects of long-term caffeine consumption on the adenosine A1 receptor (A1AR) in the rat brain. PROCEDURES: Sixteen adult, male rats underwent five positron emission tomography (PET) scans with the highly selective A1AR radioligand [(18)F]CPFPX in order to determine A1AR availability...
September 11, 2017: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
https://www.readbyqxmd.com/read/28815276/determination-of-89-drugs-and-other-micropollutants-in-unfiltered-wastewater-and-freshwater-by-lc-ms-ms-an-alternative-sample-preparation-approach
#9
Alexandros G Asimakopoulos, Pranav Kannan, Sean Higgins, Kurunthachalam Kannan
A liquid chromatography-triple quadrupole-tandem mass spectrometry (LC-qQq-MS/MS) method was developed for simultaneous determination of 89 legal neuropsychiatric pharmaceuticals and illicit drugs (both parent compounds and metabolites) and other micropollutants in unfiltered wastewater and freshwater. The target chemicals fall under the classes of amphetamine-type stimulants, cocaine compounds, opiates and opioids, benzodiazepines, lysergic compounds, antipsychotics, anesthetics, antiepileptics, antidepressants, sympathomimetics, cannabinoids, blood thinners, antihistamines, β-blockers, caffeine derivatives, nicotine derivatives, z-drugs, new designer drugs, and Alzheimer medications...
October 2017: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/28753475/presenilin-1-mutation-decreases-both-calcium-and-contractile-responses-in-cerebral-arteries
#10
Xavier Toussay, Jean-Luc Morel, Nathalie Biendon, Lolita Rotureau, François-Pierre Legeron, Marie-Charlotte Boutonnet, Yoon H Cho, Nathalie Macrez
Mutations or upregulation in presenilin 1 (PS1) gene are found in familial early-onset Alzheimer's disease or sporadic late-onset Alzheimer's disease, respectively. PS1 has been essentially studied in neurons and its mutation was shown to alter intracellular calcium (Ca(2+)) signals. Here, we showed that PS1 is expressed in smooth muscle cells (SMCs) of mouse cerebral arteries, and we assessed the effects of the deletion of exon 9 of PS1 (PS1dE9) on Ca(2+) signals and contractile responses of vascular SMC. Agonist-induced contraction of cerebral vessels was significantly decreased in PS1dE9 both in vivo and ex vivo...
June 24, 2017: Neurobiology of Aging
https://www.readbyqxmd.com/read/28582855/diabetes-and-alzheimer-s-disease-can-tea-phytochemicals-play-a-role-in-prevention
#11
Warnakulasuriya M A D B Fernando, Geeshani Somaratne, Kathryn G Goozee, Shehan Williams, Harjinder Singh, Ralph N Martins
Dementia and diabetes mellitus are prevalent disorders in the elderly population. While recognized as two distinct diseases, diabetes has more recently recognized as a significant contributor to risk for developing dementia, and some studies make reference to type 3 diabetes, a condition resulting from insulin resistance in the brain. Alzheimer's disease, the most common form of dementia, and diabetes, interestingly, share underlying pathological processes, commonality in risk factors, and, importantly, pathways for intervention...
2017: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/28507563/can-coffee-consumption-lower-the-risk-of-alzheimer-s-disease-and-parkinson-s-disease-a-literature-review
#12
Regina Wierzejska
In light of the fact that the number of elderly citizens in society is steadily increasing, the search for dietary factors which might prolong mental agility is growing in significance. Coffee, together with its main ingredient, caffeine, has been the focus of much attention from various researchers, as data on its beneficial effects on human health continue to accumulate. Most reports indicate that moderate coffee consumption may in fact lower the risk for common neurodegenerative conditions, i.e. Alzheimer's and Parkinson's diseases...
April 1, 2017: Archives of Medical Science: AMS
https://www.readbyqxmd.com/read/28317317/the-neuroprotective-effects-of-caffeine-in-neurodegenerative-diseases
#13
REVIEW
Mahshad Kolahdouzan, Mazen J Hamadeh
Caffeine is the most widely used psychostimulant in Western countries, with antioxidant, anti-inflammatory and anti-apoptotic properties. In Alzheimer's disease (AD), caffeine is beneficial in both men and women, in humans and animals. Similar effects of caffeine were observed in men with Parkinson's disease (PD); however, the effect of caffeine in female PD patients is controversial due to caffeine's competition with estrogen for the estrogen-metabolizing enzyme, CYP1A2. Studies conducted in animal models of amyotrophic lateral sclerosis (ALS) showed protective effects of A2A R antagonism...
April 2017: CNS Neuroscience & Therapeutics
https://www.readbyqxmd.com/read/28266613/screening-with-an-nmnat2-msd-platform-identifies-small-molecules-that-modulate-nmnat2-levels-in-cortical-neurons
#14
Yousuf O Ali, Gillian Bradley, Hui-Chen Lu
Nicotinamide mononucleotide adenylyl transferase 2 (NMNAT2) is a key neuronal maintenance factor and provides potent neuroprotection in numerous preclinical models of neurological disorders. NMNAT2 is significantly reduced in Alzheimer's, Huntington's, Parkinson's diseases. Here we developed a Meso Scale Discovery (MSD)-based screening platform to quantify endogenous NMNAT2 in cortical neurons. The high sensitivity and large dynamic range of this NMNAT2-MSD platform allowed us to screen the Sigma LOPAC library consisting of 1280 compounds...
March 7, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28177691/caffeine-intake-increases-plasma-ketones-an-acute-metabolic-study-in-humans
#15
RANDOMIZED CONTROLLED TRIAL
Camille Vandenberghe, Valérie St-Pierre, Alexandre Courchesne-Loyer, Marie Hennebelle, Christian-Alexandre Castellano, Stephen C Cunnane
Brain glucose uptake declines during aging and is significantly impaired in Alzheimer's disease. Ketones are the main alternative brain fuel to glucose so they represent a potential approach to compensate for the brain glucose reduction. Caffeine is of interest as a potential ketogenic agent owing to its actions on lipolysis and lipid oxidation but whether it is ketogenic in humans is unknown. This study aimed to evaluate the acute ketogenic effect of 2 doses of caffeine (2.5; 5.0 mg/kg) in 10 healthy adults...
April 2017: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/28091956/does-caffeine-influence-the-anticholinesterase-and-antioxidant-properties-of-donepezil-evidence-from-in-vitro-and-in-vivo-studies
#16
Ganiyu Oboh, Opeyemi Babatunde Ogunsuyi, Oluwaseyi Emmanuel Olonisola
Caffeine is adjudged world's most consumed pharmacologically active food component. With reports of the potential cognitive enhancing properties of caffeine, we sought to investigate if caffeine can influence the anticholinesterase and antioxidant properties of donepezil-a selective acetylcholinesterase (AChE) inhibitor used in the management of Alzheimer's disease (AD). In vitro, we investigated the effect of donepezil (DON), caffeine (CAF) and their various combinations on the activity of AChE in rat brain homogenate, as well as determined their antioxidant properties...
April 2017: Metabolic Brain Disease
https://www.readbyqxmd.com/read/28074613/health-benefits-of-methylxanthines-in-neurodegenerative-diseases
#17
REVIEW
Ainhoa Oñatibia-Astibia, Rafael Franco, Eva Martínez-Pinilla
Methylxanthines (MTXs) are consumed by almost everybody in almost every area of the world. Caffeine, theophylline and theobromine are the most well-known members of this family of compounds; they are present, inter alia, in coffee, tea, cacao, yerba mate and cola drinks. MTXs are readily absorbed in the gastrointestinal tract and are able to penetrate into the central nervous system, where they exert significant psychostimulant actions, which are more evident in acute intake. Coffee has been paradigmatic, as its use was forbidden in many diseases, however, this negative view has radically changed; evidence shows that MTXs display health benefits in diseases involving cell death in the nervous system...
June 2017: Molecular Nutrition & Food Research
https://www.readbyqxmd.com/read/27793638/tau-hyperphosphorylation-in-the-brain-of-ob-ob-mice-is-due-to-hypothermia-importance-of-thermoregulation-in-linking-diabetes-and-alzheimer-s-disease
#18
Maud Gratuze, Noura B El Khoury, Andréanne Turgeon, Carl Julien, François Marcouiller, Françoise Morin, Robert A Whittington, André Marette, Frédéric Calon, Emmanuel Planel
Over the last few decades, there has been a significant increase in epidemiological studies suggesting that type 2 diabetes (T2DM) is linked to a higher risk of Alzheimer's disease (AD). However, how T2DM affects AD pathology, such as tau hyperphosphorylation, is not well understood. In this study, we investigated the impact of T2DM on tau phosphorylation in ob/ob mice, a spontaneous genetic model of T2DM. Tau phosphorylation at the AT8 epitope was slightly elevated in 4-week-old ob/ob mice while 26-week-old ob/ob mice exhibited tau hyperphosphorylation at multiple tau phospho-epitopes (Tau1, CP13, AT8, AT180, PHF1)...
February 2017: Neurobiology of Disease
https://www.readbyqxmd.com/read/27629410/caffeine-blocks-hiv-1-tat-induced-amyloid-beta-production-and-tau-phosphorylation
#19
Mahmoud L Soliman, Jonathan D Geiger, Xuesong Chen
The increased life expectancy of people living with HIV-1 who are taking effective anti-retroviral therapeutics is now accompanied by increased Alzheimer's disease (AD)-like neurocognitive problems and neuropathological features such as increased levels of amyloid beta (Aβ) and phosphorylated tau proteins. Others and we have shown that HIV-1 Tat promotes the development of AD-like pathology. Indeed, HIV-1 Tat once endocytosed into neurons can alter morphological features and functions of endolysosomes as well as increase Aβ generation...
March 2017: Journal of Neuroimmune Pharmacology: the Official Journal of the Society on NeuroImmune Pharmacology
https://www.readbyqxmd.com/read/27563362/potential-role-of-caffeine-in-the-treatment-of-parkinson-s-disease
#20
Mohsin H K Roshan, Amos Tambo, Nikolai P Pace
Parkinson's disease [PD] is the second most common neurodegenerative disorder after Alzheimer's disease, affecting 1% of the population over the age of 55. The underlying neuropathology seen in PD is characterised by progressive loss of dopaminergic neurons in the substantia nigra pars compacta with the presence of Lewy bodies. The Lewy bodies are composed of aggregates of α-synuclein. The motor manifestations of PD include a resting tremor, bradykinesia, and muscle rigidity. Currently there is no cure for PD and motor symptoms are treated with a number of drugs including levodopa [L-dopa]...
2016: Open Neurology Journal
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