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https://www.readbyqxmd.com/read/29667758/synthesis-of-enantiomerically-enriched-drug-precursors-by-lactobacillus-paracasei-bd87e6-as-a-biocatalyst
#1
Selda Öksüz, Engin Şahin, Enes Dertli
Global sales of single enantiomeric drug products are growing at an alarming rate every year. A total of 7 bacterial strains were screened for their ability to reduce acetophenones to its corresponding alcohol. Among these strain Lactobacillus paracasei BD87E6 was found to be the most successful biocatalyst to reduce the ketones to the corresponding alcohols. The reaction conditions were systematically optimized for the reducing agent Lactobacillus paracasei BD87E6, which showed high enantioselectivity and conversion for the bioreduction...
April 18, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29667108/5-hydroxytryptamine-receptor-6-antagonist-sb258585-exerts-neuroprotection-in-a-rat-model-of-streptozotocin-induced-alzheimer-s-disease
#2
Nasrin Hashemi-Firouzi, Siamak Shahidi, Sara Soleimani-Asl, Alireza Komaki
Alzheimer's disease (AD) is a neurodegenerative disorder characterized by progressive memory decline. It has been suggested that 5-hydroxytryptamine receptor 6 (5-HT6R) might be involved in AD pathology. The aim of this study was to evaluate the effect of a 5-HT6R antagonist on cognition, learning, memory, and hippocampal apoptosis in an experimental rat model of AD. AD was induced by intracerebroventricular (icv) administration of streptozotocin (STZ; 3 mg/kg, 10 μL, twice). Adult, male rats were divided into the following groups: control, sham, AD (saline treatment, 1 μL icv for 30 days), and AD + SB258585 (5-HT6R antagonist, 1 μg/μL icv for 30 days)...
April 17, 2018: Metabolic Brain Disease
https://www.readbyqxmd.com/read/29666700/oil-palm-phenolics-inhibit-the-in-vitro-aggregation-of-%C3%AE-amyloid-peptide-into-oligomeric-complexes
#3
Robert P Weinberg, Vera V Koledova, Hyeari Shin, Jennifer H Park, Yew Ai Tan, Anthony J Sinskey, Ravigadevi Sambanthamurthi, ChoKyun Rha
Alzheimer's disease is a severe neurodegenerative disease characterized by the aggregation of amyloid- β peptide (A β ) into toxic oligomers which activate microglia and astrocytes causing acute neuroinflammation. Multiple studies show that the soluble oligomers of A β 42 are neurotoxic and proinflammatory, whereas the monomers and insoluble fibrils are relatively nontoxic. We show that A β 42 aggregation is inhibited in vitro by oil palm phenolics (OPP), an aqueous extract from the oil palm tree (Elaeis guineensis) ...
2018: International Journal of Alzheimer's Disease
https://www.readbyqxmd.com/read/29665389/application-of-pectin%C3%A2-zinc-oxide-hybrid-nanocomposite-in-the-delivery-of-a-hydrophilic-drug-and-a-study-of-its-isotherm-kinetics-and-release-mechanism
#4
Arun K Kodoth, Vivek M Ghate, Shaila A Lewis, B Vishalakshi
Pectin-based gel and its nanocomposite with zinc oxide have been compared for their capacity to release Donepezil for the possible use as an implantable drug delivery platform for the treatment of Alzheimer's disease. Adsorption capacities of the samples were determined as a function of pH, temperatures, concentrations of the drug, and the mass of the adsorbent. The nanocomposite exhibited significant adsorption compared to the parent gel. Adsorption data for the nanocomposite system fits well with Langmuir model and followed pseudo-first order kinetics, while that of the parent polymeric system followed pseudo-second-order kinetics...
April 14, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29665128/a-role-for-astrocyte-derived-amyloid-%C3%AE-peptides-in-the-degeneration-of-neurons-in-an-animal-model-of-temporal-lobe-epilepsy
#5
A Kodam, D Ourdev, M Maulik, J Hariharakrishnan, M Banerjee, Y Wang, S Kar
Kainic acid, an analogue of the excitatory neurotransmitter glutamate, can trigger seizures and neurotoxicity in the hippocampus and other limbic structures in a manner that mirrors the neuropathology of human temporal lobe epilepsy (TLE). However, the underlying mechanisms associated with the neurotoxicity remain unclear. Since amyloid-β (Aβ) peptides, which are critical in the development of Alzheimer's disease, can mediate toxicity by activating glutamatergic NMDA receptors, it is likely that the enhanced glutamatergic transmission that renders hippocampal neurons vulnerable to kainic acid treatment may involve Aβ peptides...
April 17, 2018: Brain Pathology
https://www.readbyqxmd.com/read/29663890/methodologies-related-to-computational-models-in-view-of-developing-anti-alzheimer-drugs-an-overview
#6
Kirtee Baheti, Mayura Ajay Kale
BACKGROUND: Since last two decades, there has been more focus on the development strategies related to Anti-Alzheimer's drug research. This may be attributed to the fact that most of the Alzheimer's cases are still mostly unknown except for a few cases, where genetic differences have been identified. With the progress of the disease, the symptoms involve intellectual deterioration, memory impairment, abnormal personality and behavioural patterns, confusion, aggression, mood swings, irritability Current therapies available for this disease give only symptomatic relief and do not focus on manipulations of biololecular processes...
April 17, 2018: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/29663817/inhibitory-interneurons-in-alzheimer-s-disease
#7
G Vargova, T Vogels, Z Kostecka, T Hromadka
Alzheimer's disease is currently the most common neurodegenerative disorder, characterized by distinct cognitive and sensory deficits. The underlying pathogenetic mechanisms, however, still remain elusive. How the molecular and morphological changes associated with Alzheimer's disease affect information processing in neuronal circuits and translate into cognitive dysfunction is unclear. Inhibitory interneurons have recently emerged as one of the earliest and important culprits in mediating dysfunction of neuronal circuits in neurodegeneration...
2018: Bratislavské Lekárske Listy
https://www.readbyqxmd.com/read/29660941/brimapitide-reduced-neuronal-stress-markers-and-cognitive-deficits-in-5xfad-transgenic-mice
#8
Sarah Gourmaud, Priscilla Thomas, Sylvie Thomasseau, Marion Tible, Claire Abadie, Claire Paquet, Jacques Hugon
Alzheimer's disease (AD) is characterized by accumulations of amyloid-β (Aβ42) and hyperphosphorylated tau proteins, associated with neuroinflammation, synaptic loss, and neuronal death. Several studies indicate that c-Jun N-terminal kinase (JNK) is implicated in the pathological features of AD. We have investigated in 5XFAD mice, the therapeutic effects of Brimapitide, a JNK-specific inhibitory peptide previously tested with higher concentrations in another AD model (TgCRND8). Three-month-old 5XFAD and wild-type littermate mice were treated by intravenous injections of low doses (10 mg/kg) of Brimapitide every 3 weeks, for 3 or 6 months (n = 6-9 per group)...
April 11, 2018: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/29660939/aberrant-cortical-event-related-potentials-during-associative-learning-in-rat-models-for-presymptomatic-stages-of-alzheimer-s-disease
#9
Bardia Nouriziabari, Susmita Sarkar, Stephanie E Tanninen, Robert D Dayton, Ronald L Klein, Kaori Takehara-Nishiuchi
Trace eyeblink conditioning is a hippocampus-dependent associative learning paradigm which is impaired in patients with Alzheimer's disease (AD) and animal AD models. Learning in this paradigm accompanies changes in oscillatory activity in forebrain regions, some of which are loci of pathogenic changes in prodromal AD stages. These observations motivated us to examine how cortical event-related potentials (ERPs) during this paradigm are affected by two features of the asymptomatic, AD-related brain abnormality, entorhinal tau accumulation and mild cholinergic deficit...
April 11, 2018: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/29660938/the-alzheimer-s-disease-assessment-scale-cognitive-subscale-adas-cog-modifications-and-responsiveness-in-pre-dementia-populations-a-narrative-review
#10
Jacqueline K Kueper, Mark Speechley, Manuel Montero-Odasso
The Alzheimer's Disease Assessment Scale- Cognitive Subscale (ADAS-Cog) was developed in the 1980s to assess the level of cognitive dysfunction in Alzheimer's disease. Advancements in the research field have shifted focus toward pre-dementia populations, and use of the ADAS-Cog has extended into these pre-dementia studies despite concerns about its ability to detect important changes at these milder stages of disease progression. If the ADAS-Cog cannot detect important changes, our understanding of pre-dementia disease progression may be compromised and trials may incorrectly conclude that a novel treatment approach is not beneficial...
April 11, 2018: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/29660937/personality-modulates-the-efficacy-of-art-intervention-on-chronic-pain-in-a-population-of-patients-with-alzheimer-s-disease
#11
Isabelle Rouch, Elodie Pongan, Yohana Leveque, Barbara Tillmann, Béatrice Trombert, Jean Claude Getenet, Nicolas Auguste, Pierre Krolak-Salmon, Bernard Laurent, Jean-Michel Dorey
BACKGROUND: Alzheimer's disease (AD) mainly occurs in elderly individuals. Comorbidities and chronic pain are frequent in this population. Previous studies revealed that personality modulates both chronic pain (CP) andADoccurrence and evolution. Moreover, as pain treatments can induce side-effects, non-drugs treatments, such as art interventions, are interesting alternative therapies for decreasing CP in these patients. OBJECTIVE: Our aim was to assess the potential role of personality traits on art intervention efficacy for reducing CP in a population of patients with mild AD...
April 11, 2018: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/29659206/effects-of-antipsychotics-on-secular-mortality-trends-in-patients-with-alzheimer-s-disease
#12
René Ernst Nielsen, Jan B Valentin, Annette Lolk, Kjeld Andersen
OBJECTIVE: To investigate secular changes in mortality rates between patients with Alzheimer's disease (AD) and the general population as well as changes in antipsychotic drug treatment and the association between drug treatment and mortality in patients with AD in Denmark during a 12-year study period. METHODS: This nationwide, retrospective cohort study identified all-cause mortality in all Danish patients with incident ICD-10-defined AD from 2000 through 2011...
April 3, 2018: Journal of Clinical Psychiatry
https://www.readbyqxmd.com/read/29658441/efficacy-of-transcranial-direct-current-stimulation-combined-with-cognitive-training-in-the-treatment-of-apathy-in-patients-with-alzheimer-s-disease-study-protocol-for-a-randomized-trial
#13
Nguyen Jean-Paul, Claire Boutoleau-Bretonniere, Jean-Pascal Lefaucheur, Alcira Suarez, Helene Gaillard, Guillaume Chapelet, Sebastien Abad, Aurelien Van Langhenhove, Julian Nizard, Laure de Decke
BACKGROUND: Apathy, commonly defined as loss of motivation, is a symptom frequently encountered in Alzheimer's disease (AD). The treatment of apathy remains challenging in the absence of any truly effective medications. Transcranial magnetic stimulation (rTMS) or transcranial direct current stimulation (tDCS) can improve cognitive disorders, but do not appear to improve apathy. Isolated cognitive training also appears to have no effect on apathy. We propose to test the efficacy of a new procedure for the treatment of apathy in AD patients consisting of a combination of tDCS and cognitive training, based on the latest guidelines for the design of therapeutic trials in this field...
April 16, 2018: Reviews on Recent Clinical Trials
https://www.readbyqxmd.com/read/29656989/substituent-effect-of-n-benzylated-gramine-derivatives-that-prevent-the-pp2a-inhibition-and-dissipate-the-neuronal-ca-2-overload-as-a-multitarget-strategy-for-the-treatment-of-alzheimer-s-disease
#14
Dorleta Gonzalez, Raquel L Arribas, Lucia Viejo, Rocio Lajarin-Cuesta, Cristobal de Los Rios
Following the premises of the multitarget-directed ligands approach for the drug R&D against neurodegenerative diseases, where Alzheimer's disease (AD) outstands, we have synthesized and evaluated analogues of the gramine derivative ITH12657 (1-benzyl-5-methyl-3-(piperidin-1-ylmethyl-1H-indole, 2), which had shown important neuroprotective properties, such as blocking effect of voltage-gated Ca2+ channels (VGCC), and prevention of phosphoprotein phosphatase 2A (PP2A) inhibition. The new analogues present different substitutions at the pending phenyl ring, what slightly modified their pharmacological characteristics...
April 9, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29656360/dietary-vitamin-e-status-dictates-oxidative-stress-outcomes-by-modulating-effects-of-fish-oil-supplementation-in-alzheimer-disease-model-app-swe-ps1-de9-mice
#15
Shengqi Dong, Xiaochen Huang, Jie Zhen, Nicholas Van Halm-Lutterodt, JiaJia Wang, Cui Zhou, Linhong Yuan
Quite a number of studies have examined the effects of fish oil supplementation on cognitive performance in different transgenic animal models of Alzheimer's disease (AD). However, inconsistent and controversial outcomes have been derived from these experiments. In order to investigate whether the beneficial effect of fish oil supplementation on cognition was dietary VE status associated, fish oil dietary intervention was carried out in transgenic APPswe /PS1dE9 (APP/PS1) mice. Control mice (C57BL/6J mice) were fed a normal control diet...
April 14, 2018: Molecular Neurobiology
https://www.readbyqxmd.com/read/29655652/protective-role-of-rosmarinic-acid-on-amyloid-beta-42-induced-echoic-memory-decline-implication-of-oxidative-stress-and-cholinergic-impairment
#16
Deniz Kantar Gok, Enis Hidisoglu, Guzide Ayse Ocak, Hakan Er, Alev Duygu Acun, Piraye Yargıcoglu
In the present study, we examined whether rosmarinic acid (RA) reverses amyloid β (Aβ) induced reductions in antioxidant defense, lipid peroxidation, cholinergic damage as well as the central auditory deficits. For this purpose, Wistar rats were randomly divided into four groups; Sham(S), Sham + RA (SR), Aβ42 peptide (Aβ) and Aβ42 peptide + RA (AβR) groups. Rat model of Alzheimer was established by bilateral injection of Aβ42 peptide (2,2 nmol/10 μl) into the lateral ventricles. RA (50 mg/kg, daily) was administered orally by gavage for 14 days after intracerebroventricular injection...
April 12, 2018: Neurochemistry International
https://www.readbyqxmd.com/read/29653407/a-new-alzheimer-s-disease-cell-model-using-b-cells-to-induce-beta-amyloid-plaque-formation-and-increase-tnf-alpha-expression
#17
Mehrouz Dezfulian
Different cell models have been developed for the study of Alzheimer's disease (AD) pathways. The neuronal dysfunction and cell death mechanisms that are commonly found in this disease are due to the production of high levels of cytokines and the formation of amyloid plaques. In the cell model introduced in the present study, the production of these two important factors is induced by using B cells from an AD patient. The B cells of an Alzheimer's patient and a normal control were immortalized by using EBV (Epstein-Barr virus) to produce a lymphoblastoid cell line (LCL)...
April 10, 2018: International Immunopharmacology
https://www.readbyqxmd.com/read/29651948/therapeutic-potential-of-multifunctional-tacrine-analogues
#18
Maja Przybylowska, Szymon Kowalski, Krystyna Dzierzbicka, Iwona Inkielewicz-Stepniak
Tacrine is a potent inhibitor of cholinesterases (acetylcholinesterase and butyrylcholinesterase) that shows limiting clinical application by liver toxicity. In spite of this, analogues of tacrine are considered as model inhibitor of cholinesterases in the therapy of Alzheimer's disease. The interest in these compounds is mainly related to a high variety of their structure and biological properties. In the present review, we have described the role of cholinergic transmission and treatment strategies in Alzheimer's disease as well as the synthesis and biological activity of several recently developed classes of multifunctional tacrine analogues and hybrids, which consist a new paradigm to treat Alzheimer's disease...
April 11, 2018: Current Neuropharmacology
https://www.readbyqxmd.com/read/29651884/kinetic-and-structural-studies-on-the-interactions-of-torpedo-californica-acetylcholinesterase-with-two-donepezil-like-rigid-analogues
#19
Rosanna Caliandro, Alessandro Pesaresi, Luca Cariati, Antonio Procopio, Manuela Oliverio, Doriano Lamba
Acetylcholinesterase inhibitors were introduced for the symptomatic treatment of Alzheimer's disease (AD). Among the currently approved inhibitors, donepezil (DNP) is one of the most preferred choices in AD therapy. The X-ray crystal structures of Torpedo californica AChE in complex with two novel rigid DNP-like analogs, compounds 1 and 2, have been determined. Kinetic studies indicated that compounds 1 and 2 show a mixed-type inhibition against TcAChE, with Ki values of 11.12 ± 2.88 and 29.86 ± 1...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29644989/the-palliative-care-in-dementia-context-health-professionals-point-of-view-about-advantages-and-resistances
#20
Sabina Zapponi, Maria Chiara Ascari, Erjona Feracaku, Silvia Masin, Paola Paglia, Roberta Petroccione, Ana Pinzaru, Chiara Foà, Giovanna Artioli, Leopoldo Sarli
BACKGROUND AND AIM: The 38/2010 law has expanded the provision of palliative care to patients with chronic-degenerative diseases. The ISTAT data show that 60% of the dying population is suffering from these diseases and could, according to the literature review, benefit particularly from such treatments. This study investigates the point of view of healthcare professionals, working in the context of dementia, regarding the knowledge and application of palliative care in the field of dementia...
March 26, 2018: Acta Bio-medica: Atenei Parmensis
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