Editors Choice Article | Detecting Non-cognitive Features of Prodromal Neurodegenerative Diseases

 

Journal Name: Current Aging Science

Author(s): Alon Seifan, Christine A. Ganzer*, Krista Ryon, Michael Lin, Rahman Mahmudur, Henriquez Adolfo, Cindy Shih, Alan R. Jacobs, Molly Greenwald, Richard S. Isaacson.

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Background: Prodromal Neurodegenerative Disease (ND) due to tauopathies such as Alzheimer’s Disease (AD) and Synucleinopathies (SN) such as Parkinson’s Disease (PD) and Dementia with Lewy Bodies (DLB) present subtly. Although ND are considered cognitive disorders, in fact ND present with behavioral and even medical symptomatology years to decades prior to the onset of cognitive changes. Recognizing prodromal ND syndromes is a public health priority because ND is common, disabling and expensive. Diagnosing prodromal ND in real world clinical settings is challenging because ND of the same pathology can present with different symptoms in different people. Individual variability in nature and variability in nurture across the life course influence how ND pathology manifests clinically. The objective of this study was to describe how non-cognitive symptoms from behavioral, medical, neurological and psychiatric domains cluster in prodromal and early stages of ND.

Methods: This was an observational study of patients receiving routine clinical care for memory disorders. All patients receiving a standardized evaluation including complete neurological history and examination and standardized brief neuropsychological testing. A Principal Component Analysis (PCA) considering emotion, motor, sensory and sleep factors was performed on the entire sample of patients in order to identify co-occurring symptom clusters. All patients received a consensus diagnosis adjudicated by at least two dementia experts. Patients were grouped into Cognitively Normal, Detectable Cognitive Impairment, and Mild Cognitive Impairment categories due to AD and/or PD/LBD or NOS pathology. Symptom cluster scores were compared between clinical diagnostic groups. Read out full article at: http://www.eurekaselect.com/169580/article

Editor’s Choice Article | Functional Cross-Talk between Adenosine and Metabotropic Glutamate Receptors

 

Journal Name: Current Neuropharmacology

Author(s): David Agustín León-Navarro, José Luis Albasanz, Mairena Martín*.

 

G-protein coupled receptors are transmembrane proteins widely expressed in cells and their transduction pathways are mediated by controlling second messenger levels through different G-protein interactions. Many of these receptors have been described as involved in the physiopathology of neurodegenerative diseases and even considered as potential targets for the design of novel therapeutic strategies. Endogenous and synthetic allosteric and orthosteric selective ligands are able to modulate GPCRs at both gene and protein expression levels and can also modify their physiological function. GPCRs that coexist in the same cells can homo- and heteromerize, therefore, modulating their function. Adenosine receptors are GPCRs which stimulate or inhibit adenylyl cyclase activity through Gi/Gs protein and are involved in the control of neurotransmitter release as glutamate. In turn, metabotropic glutamate receptors are also GPCRs which inhibit adenylyl cyclase or stimulate phospholipase C activities through Gi or Gq proteins, respectively. In recent years, evidence of crosstalk mechanisms between different GPCRs have been described. The aim of the present review was to summarize the described mechanisms of interaction and crosstalking between adenosine and metabotropic glutamate receptors, mainly of group I, in both in vitro and in vivo systems, and their possible use for the design of novel ligands for the treatment of neurodegenerative diseases. Read out full article at: http://www.eurekaselect.com/161279/article

Editor’s Choice Article | Unequal Absorption of Radiolabeled and Nonradiolabeled Drug from the Oral Dose Leads to Incorrect Estimates of Drug Absorption and Circulating Metabolites in a Mass Balance Study

Journal Name: Drug Metabolism Letters

Author(s): Ryan H. Takahashi*, Jae H. Chang, Jodie Pang, Xiaorong Liang, Shuguang Ma.

 

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Mass balance studies conducted using radiolabeled material (14C or 3H) definitively characterize the Absorption, Metabolism, and Excretion (AME) of a drug. A critical aspect of these studies is that the radiotracer maintains its proportion to total drug from its administration to its complete elimination from the body. In the study of GDC-0276 in beagle dogs, we observed that the 14C radiotracer proportion (specific activity) varied through the study.

High resolution-accurate mass spectrometric measurements of 12C and 14C isotopes of GDC- 0276 and its metabolites in plasma and excreta samples were used to determine the apparent specific activities, which were higher than the specific activity of the dosing formulation. Drug concentrations were adjusted to the observed specific activities to correct the readouts for GDC-0276 AME and PK. Read out full article at:  http://www.eurekaselect.com/167902/article

 

Editor’s Choice Article | Design, Microwave Assisted Organic Synthesis and Molecular Docking Studies of Some 4 – (3H)-Quinazolinone Derivatives as Inhibitors of Colchicine- Binding Site of Tubulin

Author(s): Rakesh D. Amrutkar*, Mahendra S. Ranawat.

 

Currently, new chemical entities developed as anticancer agents against tubulin as a protein target. The present work, a quinazoline derivatives were used to design and synthesized by microwave irradiation as an anticancer agent through selective inhibitors of colchicinebinding site of tubulin by the molecular docking of quinazoline derivatives using Schrödinger, LLC, New York, NY, 2017. Read out full article here: http://www.eurekaselect.com/166586/article

 

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Editor’s Choice Article | Graphene Quantum Dots in Electrochemical Sensors/Biosensors

Author(s): Farnoush Faridbod*, Afsaneh L. Sanati.

 

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Graphene and its derivatives, as most promising carbonic nanomaterials have been widely used in design and making electrochemical sensors and biosensors. Graphene quantum dots are one of the members of this family which have been mostly known as fluorescent nanomaterials and found extensive applications due to their remarkable optical properties. Quantum confinement and edge effects in their structures also cause extraordinary electrochemical properties. Read out full article here: http://www.eurekaselect.com/160545/article

Editor’s Choice Article | Synthesis, Molecular Modeling and Biological Evaluation of 5-arylidene- N,N-diethylthiobarbiturates as Potential α-glucosidase Inhibitors

 

Author(s): Momin Khan*, Sehrish Khan, Amir Ul Mulk, Anis Ur Rahman, Abdul Wadood, Sulaiman Shams, Muhammad Ashraf, Jameel Rahman, Iltaf Khan, Abdul Hameed, Zahid Hussain, Abbas Khan, Khair Zaman, Khalid M. Khan, Shahnaz Perveen.

Journal Name: Medicinal Chemistry

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Barbituric acid derivatives are a versatile group of compounds which are identified as potential pharmacophores for the treatment of anxiety, epilepsy and other psychiatric disorders. They are also used as anesthetics and have sound effects on the motor and sensory functions. Barbiturates are malonylurea derivatives with a variety of substituents at C-5 position showing resemblance with nitrogen and sulfur containing compounds like thiouracil which exhibited potent anticancer and antiviral activities. Recently, barbituric acid derivatives have also received great interest for applications in nanoscience. Read out full article here: http://www.eurekaselect.com/165349/article

Editor’s Choice Article | Diastasis Recti Abdominis-diagnosis, Risk Factors, Effect on Musculoskeletal Function, Framework for Treatment and Implications for the Pelvic Floor

Author(s): Laura Anne Werner*, Marcy Dayan.

Journal Name: Current Women`s Health Reviews

 

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Diastasis Recti Abdominis (DRA) can occur during pregnancy and postpartum. It is defined as an increase of the inter-recti distance (IRD) beyond normal values. The diagnosis of DRA is inconsistent within the literature and varies depending on measurement instrument and activity during measurement (rest versus active curl-up). DRA is characterized by the stretching of linea alba (LA) and contributes to a protrusion of the anterior abdominal wall due to increased laxity in the myofascial system that supports abdominal viscera. DRA has been postulated to affect lumbopelvic support and function due to laxity of the LA and altered angle of muscle insertion, but recent studies have not confirmed this. Risk factors for the development of DRA have been investigated in pregnancy to 12-months postpartum. Read out full article here: http://www.eurekaselect.com/160043/article

Editor’s Choice Article | The Future of Biogas Production in Cameroon: Prospects, Challenges and Opportunities

Author(s): Erasmus Muh*, Fouzi Tabet, Sofiane Amara.

 

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Abstract:

Cameroon is blessed with a vast potential of energy resources. However, their level of valorization is deplorable causing acute energy challenges. Consequently, most Cameroonians, mainly rural dwellers are dependent on traditional biomass and petroleum products for their basic energy needs despite their associated adverse health and the environmental impacts. Thus, there is a need for alternative, affordable and reliable energy sources to meet this energy gap. This study, therefore, reviews and assesses the prospects and sustainability of biogas production in Cameroon. Read out full article here: http://www.eurekaselect.com/165655/article

Editor’s Choice Article | Chemistry and Biology of Secondary Metabolites from Aspergillus Genus

Author(s): Xiaolei Zhang, Zhi Li, Jiangtao Gao*.

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Abstract: Aspergillus is a genus of ubiquitous fungi that are therapeutically important because the genus produces a wide range of structurally diverse secondary metabolites that are of highly considerable interest to both scientific research community and pharmaceutical industry. Genome sequencing results have indicated that chemical diversity of secondary metabolites is much larger in each species than previously thought.

This review summarizes a total of 315 new secondary metabolites of Aspergillus reported from 2015 to 2017 and demonstrates the therapeutical potential of this genus by introducing their unique chemical structures and excellent bioactivities from this genus. Read out full article here: http://www.eurekaselect.com/161751/article

 

Editor’s Choice Article | Statins and the Brain: More than Lipid Lowering Agents?

Journal Name: Current Neuropharmacology

Author(s): Anna Fracassi, Martina Marangoni, Pamela Rosso, Valentina Pallottini, Marco Fioramonti, Silvia Siteni, Marco Segatto*.

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Abstract:

Background: Statins represent a class of medications widely prescribed to efficiently treat dyslipidemia. These drugs inhibit 3-βhydroxy 3β-methylglutaryl Coenzyme A reductase (HMGR), the rate-limiting enzyme of mevalonate (MVA) pathway. Besides cholesterol, MVA pathway leads to the production of several other compounds, which are essential in the regulation of a plethora of biological activities, including in the central nervous system. For these reasons, statins are able to induce pleiotropic actions, and acquire increased interest as potential and novel modulators in brain processes, especially during pathological conditions.

Objective: The purpose of this review is to summarize and examine the current knowledge about pharmacokinetic and pharmacodynamic properties of statins in the brain. In addition, effects of statin on brain diseases are discussed providing the most up-to-date information.

Methods: Relevant scientific information was identified from PubMed database using the following keywords: statins and brain, central nervous system, neurological diseases, neurodegeneration, brain tumors, mood, stroke.

Results: 315 scientific articles were selected and analyzed for the writing of this review article. Several papers highlighted that statin treatment is effective in preventing or ameliorating the symptomatology of a number of brain pathologies. However, other studies failed to demonstrate a neuroprotective effect.

Conclusion: Even though considerable research studies suggest pivotal functional outcomes induced by statin therapy, additional investigation is required to better determine the pharmacological effectiveness of statins in the brain, and support their clinical use in the management of different neuropathologies.

 

 

Read out more at: http://www.eurekaselect.com/153651/article

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