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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Abstract:

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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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

Editor’s Choice Article | Trends of Clinical Trials for Drug Development in Rare Diseases

Author(s): Ryuichi Sakate, Akiko Fukagawa, Yuri Takagaki, Hanayuki Okura, Akifumi Matsuyama*.

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Background: Drug development for rare diseases is challenging because it is difficult to obtain relevant data from very few patients. It must be informative to grasp current status of clinical trials for drug development in rare diseases.

Objective: Clinical trials in rare diseases are to be outlined and compared among the US, EU and Japan.

Method: ClinicalTrials.gov (NCT, National Clinical Trial), EU Clinical Trials Register (EUCTR) and the Japan Primary Registries Network (JPRN) were analyzed. Clinical trials involving information on rare diseases and drugs were extracted by text-mining, based on the diseases and drugs derived from Orphanet and DrugBank, respectively.

Results: In total, 28,526 clinical trials were extracted, which studied 1,535 rare diseases and 1,539 drugs. NCT had the largest number of trials, involving 1,252 diseases and 1,332 drugs. EUCTR and JPRN also had registry-specific diseases (250 and 22, respectively) and drugs (172 and 29, respectively) that should not be missed. Among the 1,535 rare diseases, most diseases were studied in only a limited number of trials; 70% of diseases were studied in fewer than 10 trials, and 28% were studied in only one. Additionally, most studied rare diseases were cancer-related ones.

Conclusion: This study has revealed the characteristics of the clinical trials in rare diseases among the US, EU and Japan. The number of trials for rare diseases was limited especially for non-cancerrelated ones. This information could contribute to drug development such as drug-repositioning in rare diseases.

 

 

Read out more at: http://www.eurekaselect.com/162697/article

Editor’s Choice Article | Novel QoS Aware OLSR Protocol for Opportunistic Spectrum Access in Cognitive Radio Ad-Hoc Networks

Journal Name: International Journal of Sensors, Wireless Communications and Control

Author(s): Surjeet Balhara*, Bharati Vidyapeeth College of Engineering, New Dehli, India Priyanka Bhardwaj. Bharati Vidyapeeth College of Engineering, New Dehli, India

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Background & Objective: In the design of ad-hoc networks, potential challenge is how to route information reliably and efficiently from one node to another in high level of mobility. Moreover, remaining queuing capacity is also affected on the packet loss. Much research efforts have been consistently done to create protocols that consider minimum bandwidth, better throughput and less average delay. It is widely accepted that only quality of service (QoS) fulfillment can guarantee the requirements in ad-hoc networks and improve the overall network performance.

Conclusion and Results: This paper proposes a QoS-aware optimized link state routing protocol (QOLSR) to enhance data transmission efficiency in cognitive radio ad-hoc networks (CRAHNs). The proposed algorithm utilizes link quality estimation metric and provides best end-to-end paths based on generalization of Dijkstra’s algorithm. We implement two routing algorithms, AODV and OLSR and compare their performance. Simulation is performed using NS-2.35 and the results show that the proposed algorithm outperforms the existing baseline AODV routing algorithm.

 

 

Read out more at: http://www.eurekaselect.com/163454/article

Editor’s Choice Article | Serum Proteome Profiling to Identify Proteins Promoting Pathogenesis of Non-atopic Asthma

Journal Name: Protein & Peptide Letters

Author(s): Samina Ejaz, Department of Biochemistry and Biotechnology, The Islamia University of Bahawalpur, Bahawalpur, Pakistan Faiz-ul-Hassan Nasim*, Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur, Pakistan Muhammad Ashraf, Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur, Pakistan Sami Ahmad. Department of Pulmonolgy, Quaid-i-Azam Medical College, Bahawal Victoria Hospital, Bahawalpur, Pakistan

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Abstract:

Background: Asthma is the inflammatory disorder of airways highly prevalent in both, children and adults all over the world. The aim of this study was to investigate the serum proteome for the identification of proteins contributing to the pathogenesis of non-atopic asthma.

Methods: Protein expression profiling of sera from non-atopic asthmatic patients (n=73) and controls (n=99) was carried out using 1D SDS PAGE. Differentially expressed protein bands were compared with controls, cut from the gel and identified by LC-Q-TOF_MSMS analysis.

Results: Various acute phase proteins (i.e., haptoglobin, transthyretin, serum amyloid A, and serum albumin), retinol binding protein 4 (RBP4), Ig gamma-1-chain C-region, hemoglobin subunit β, complement system components (C8 gamma chain and C4-A), ApoA-1 and Ig κ chain C-region containing protein fractions were predominantly down-regulated in asthmatic patients. Similarly, a higher proportion of male patients exhibited down-regulation of all other (except albumin and C4-A containing) protein fractions as compared to female patients. However, fractions consisting of another acute phase protein, inter-alpha-trypsin heavy chain 4 (ITIH4) and complement system component C3 were up-regulated in the majority of patients.

Conclusion: Our study is the first to confirm the role of thyroxine (TTR), retinol (RBP4), cholesterol (apoA-1) transporting proteins, inflammation and its mediators in the pathogenesis of asthma. Further study may help to improve diagnosis and plan better treatment strategies.

 

 

Read out more at: http://www.eurekaselect.com/165657/article

 

 

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