Most Accessed Articles | Synthesis and Biological Evaluation of PF-543 Derivative

 

Journal Name: Letters in Organic Chemistry

Author(s): Seon Woong Kim, Taeho Lee, Joo-Youn Lee, Sanghee Kim, Hee-Sook Jun, Eun-Young Park*, Dong Jae Baek*.

 

PF-543 has been known as a substance that strongly inhibits SK1. However, it also exhibits antineoplastic activity that is lower than other inhibitors of SK1. In this study, we compared PF-543 and synthesized a newly designed derivative of PF-543 (compound 2) in which two aromatic structures were connected in para-form. The synthesized derivative showed inhibitory effect on SK1, similar to that of PF-543. However, it was more cytotoxic to HT29, AGS, and PC3 cells than PF-543. We also carried out a docking study for SK1 and demonstrated that the synthesized derivative showed interaction with SK1 similar to PF-543. Results obtained from this study suggest that the structure of compound 2 may be well substituted for the structure of PF-543 in terms of biological activity, providing us important structural information for the design of new derivatives of PF-543. Read out full article here: http://www.eurekaselect.com/166082

 

Most Accessed Articles | A Review of Denoising Medical Images Using Machine Learning Approaches

Author(s): Prabhpreet Kaur*, Gurvinder Singh, Parminder Kaur.

Journal Name: Current Medical Imaging

 

This paper attempts to identify suitable Machine Learning (ML) approach for image denoising of radiology based medical application. The Identification of ML approach is based on (i) Review of ML approach for denoising (ii) Review of suitable Medical Denoising approach.

The review focuses on six application of radiology: Medical Ultrasound (US) for fetus development, US Computer Aided Diagnosis (CAD) and detection for breast, skin lesions, brain tumor MRI diagnosis, X-Ray for chest analysis, Breast cancer using MRI imaging. This survey identifies the ML approach with better accuracy for medical diagnosis by radiologists. The image denoising approaches further includes basic filtering techniques, wavelet medical denoising, curvelet and optimization techniques. In most of the applications, the machine learning performance is better than the conventional image denoising techniques. For fast and computational results the radiologists are using the machine learning methods on MRI, US, X-Ray and Skin lesion images. The characteristics and contributions of different ML approaches are considered in this paper. Read out full article here: http://www.eurekaselect.com/152027

 

 

Most Accessed Articles | Design, Synthesis and Characterization of Novel Urolithin Derivatives as Cholinesterase Inhibitor Agents

Author(s): Maryam Norouzbahari, Emine V. Burgaz, Tugba Ercetin, Amirhossein Fallah, Alireza Foroumadi, Loghman Firoozpour, Mustafa F. Sahin, Mustafa Gazi, Hayrettin O. Gulcan*.

Journal Name: Letters in Drug Design & Discovery

Considering the limitations of current cholinesterase inhibitor drugs for the treatment of Alzheimer’s disease, there is ongoing research activities to find out alternative drug candidates. The aryl-spacer-N-benzyl pharmacophore model has been effectively utilized to design various types of cholinesterase inhibitor molecules, including donepezil. Within this research study, we have questioned the significance of the benzyl group within this pharmacophore employing the urolithin derivatives. Urolithins are benzo[c]chromene analogue metabolites of ellagitannins, abundantly found in pomegranate and berry fruits. Read out full article here: http://www.eurekaselect.com/159057

 

Most Accessed Articles | Colorimetric Sensing of Iodide by the Competitive Interactions in the Surface of Gold Nanoparticles with the Simultaneous Aggregation/ Anti-Aggregation Mechanisms in Edible Salts

Author(s): Zolaikha Rasouli, Raouf Ghavami*.

Journal Name: Current Analytical Chemistry

 

Iodide (I-) is a vital micronutrient and its essential roles have been approved in a number of neurological activities. Therefore, there is a growing interest in developing reliable sensitive quantitative methodologies for the determination of the amount of I- in edible salt samples.

First, 2heDTC was synthesized by the mixing of equivalent amounts of pure C2H7NO and CS2 in the presence of NH4OH under vigorous stirring in an ice bath. Then, AuNPs were synthesized; the 250 mL of 1 mM HAuCl4 was put into a round-bottomed flask and was boiled vigorously by stirring for 20 min. Then, 25 mL of 38.8 mM of Na3C6H5O7 was added rapidly into this solution. The solution was heated under reflux for another 15 min. The modification of the AuNPs surface was performed with 2heDTC by proceeding with the ligand exchange reaction. To the quantification of I-, 2 µL (1mM) Hg2+ was added to 0.5 mL (50 mM) of PBS solution with pH = 5.0 containing 500 µL of 2heDTC-AuNPs, which was then maintained at optimized time for the creation of bare AuNPs. Then, the different concentrations of I- were separately added. Finally, the surface plasmon resonance (SPR) absorption bands were taken with UV-Vis spectrophotometer. Read out full article here: http://www.eurekaselect.com/161194

 

 

 

Most Accessed Articles | Extracranial-to-Intracranial Bypass for Pressor Dependent Cerebrovascular Insufficiency: Modified Classification and Representative Case

While some randomized clinical trials have reduced the indications for cerebral revascularization in the secondary prevention of ischemic stroke, a distinct subset of patients with blood pressure augmentation dependent cerebrovascular insufficiency due to large vessel occlusions remains unaddressed. With the recent paradigm shifts in acute ischemic stroke care, the role of extracranial to intracranial (EC-IC) bypass must be re-addressed when endovascular intervention is not a feasible option. We submit a refined classification of cerebrovascular insufficiency with a category called Pressor-Dependent Cerebrovascular Insufficiency (PD-CVI) for whom EC-IC bypass may be indicated. Read out full article here: http://www.eurekaselect.com/163730

 

Most Accessed Articles | Insights into the Noncoding RNA-encoded Peptides

Journal Name: Protein & Peptide Letters

Author(s): Jinchang Pan, Xiaodan Meng, Nan Jiang, Xiaofeng Jin, Chengwei Zhou, Dazhi Xu, Zhaohui Gong*.

Graphical Abstract:

Abstract:

Background: Considerable evidence has indicated that most noncoding RNA (ncRNA) transcripts act directly as functional RNAs rather than as encoded peptides. However, a recent study of ribosome occupancy reported that many large intergenic ncRNAs (lincRNAs) are bound by ribosomes, raising the possibility that they are translated into proteins. These lincRNAs contain either Internal Ribosomal Entry Sites (IRES) or short Open Reading Frames (sORFs), and other translation elements, which can be translated into peptides with physiological functions.

Conclusion: This review discusses three major types of ncRNA-encoded peptides (ncPEPs). First, microRNA(miRNA)-encoded peptides (miPEPs) are translated from their primary transcripts of miRNA genes and can promote the development of plant roots. Second, a long ncRNA(lncRNA) containing sORF encodes a 90 residues long regulatory peptide. Upon the amino acid response, the lncRNA-encoded peptide reduces the activity of mammalian Target Rapamycin complex 1 (mTORC1) and promotes muscle regeneration. Third, a circular RNA (circRNA) of the Na+/Ca2+ exchanger gene 1 (NCX1) exon 2 transcript encodes a truncated NCX1 protein exhibiting the Na+/Ca2+ exchange activity. It is also of worth noting that the majority of ncRNAs is not translated. This review summarizes the current understanding of the translatability of ncRNAs and the functions of ncPEPs in cellular processes, which may provide novel insights into the roles of ncPEPs.

 

 

Read out more at: http://www.eurekaselect.com/164529

Most Accessed Articles | Graphitization Behavior of Single Crystal Diamond for the Application in Nano-Metric Cutting

Journal Name: Current Nanoscience

Author(s): Qingshun Bai*, Zhiguo Wang, Yongbo Guo, Jiaxuan Chen, Yuanjiang Shang.

Graphical Abstract:

Abstract:

Background: Graphitization behavior of diamond has received an increasing interest in nanoscale machining of some hard and brittle materials. Diamond has always been an important and excellent tool material in cutting area. However, the graphitization of the diamond tool is inevitable when it was used in special conditions. It is indicated that the graphitization of diamond crystal has great influence on the wear resistance of diamond cutting tool. The graphitization behavior needs to be investigated extensively in nanoscale with an atomic view. Molecular dynamics simulation provides a useful tool for understanding of the graphitization mechanism of diamond. The investigation on graphitization behavior of single crystal diamond can also provide a useful reference for the application of diamond cutting tool.

Materials and Methods: In this paper, a molecular dynamics (MD) diamond crystal model is built to examine the graphitization behavior of diamond under various conditions. The sixfold ring method was employed to identify the structural characteristics of graphite and diamond. The effects of temperature and crystal orientation on the graphitization of diamond have been revealed. Considering the effect of temperature, the anisotropy of diamond graphitization against various crystal planes is presented and discussed carefully. The nano-metric cutting model of diamond tool evaluated by the sixfold ring method also proves the graphitization mechanisms in atomic view.

Results: Results indicate that the sixfold ring method is a reliable method to evaluate the graphitization behavior of diamond crystal. There exists a critical temperature of the graphitization of diamond. The results also show that {111} plane is more easy to get graphitization as compared with other crystal planes. However, {100} plane of diamond model presents the highest antigraphitization property.

Conclusion: The obtained results have provided the in-depth understanding on the wear of diamond tool in nano-metric machining and underpin the development of diamond cutting tool.

 

Read out more at: http://www.eurekaselect.com/162223

Most Accessed Articles | Applications of Nanoflowers in Biomedicine

Journal Name: Recent Patents on Nanotechnology

Author(s): Masoud Negahdary, Hossein Heli*.

Abstract:

Background: Nanotechnology has opened new windows for biomedical researches and treatment of diseases. Nanostructures with flower-like shapes (nanoflowers) which have exclusive morphology and properties have been interesting for many researchers.

Methods: In this review, various applications of nanoflowers in biomedical researches and patents from various aspects have been investigated and reviewed.

Results: Nanoflowers attracted serious attentions in whole biomedical fields such as cardiovascular diseases, microbiology, sensors and biosensors, biochemical and cellular studies, cancer therapy, healthcare, etc. The competitive power of nanoflowers against other in use technologies provides successful achievements in the progress of mentioned biomedical studies.

Conclusion: The use of nanoflowers in biomedicine leads to improving accuracy, reducing time to achieve the results, reducing costs, creating optimal treatment conditions as well as avoiding side effects of the treatment of specific diseases, and increasing functional strength.

 

 

Read out more at: http://www.eurekaselect.com/155482

Most Accessed Articles | Synthesis and Applications of Bisheterocyclic Compounds

Journal Name: Current Organic Synthesis

Author(s): Mohamad Yusuf*, Saloni Thakur.

 

 

 

Graphical Abstract:

 

Abstract:

Background: The synthesis of a variety of bisheterocyclic compounds has received a great attention not only as main chain polymers but also because many biologically active natural and synthetic products have molecular symmetry. In the synthesis of bisheterocyclic, researchers tried to extend the existing method by using a broad range of protocols to improve the various scope and limitations regarding their yield, purity and mostly on the various biological applications.

Objective: The significance of this review lies in the fact that bisheterocycles reported here display diverse chemical, structural and biological properties which makes them potential candidates for the further investigations.

Conclusion: This review article is associated with the study of the synthesis and varied applications of different bisheterocycles. These compounds have been built around the variety of intermediate chains such aliphatic, olefinic, alkynic and aromatic linkers. The presence of two heterocyclic moieties together in the same molecule either symmetrically or non-symmetrically has been found to influence the biological profiles of the resultant bis organic molecules. So, there is plenty of scope upon the development of the new bisheterocyclic in order to investigate the effect of the length and flexibility of the linkers upon their biological and other properties.

 

Read out more at: http://www.eurekaselect.com/161026

Most Accessed Articles – The Clinical and Immunological Features of Patients with Primary Antibody Deficiencies

 

Journal Name: Endocrine, Metabolic & Immune Disorders – Drug Targets

Author(s): Gholamreza Azizi, Yasser Bagheri, Marzieh Tavakol, Forough Askarimoghaddam, Kumars Porrostami, Hosein Rafiemanesh, Reza Yazdani, Fatemeh Kiaee, Sima Habibi, Kosar Abouhamzeh, Hamed Mohammadi, Mostafa Qorbani, Hassan Abolhassani, Asghar Aghamohammadi*.

Graphical Abstract:

 

Abstract:

Background: Primary antibody deficiency (PAD) comprises a range of diseases from early to late terminal B cells defects and is associated with the various clinical complications.

Methods: A total of 461 patients (311 males and 150 females) with PADs enrolled in the retrospective cohort study and for all patients’ demographic information, clinical records and laboratory data were collected to investigate clinical complications.

Results: The most prevalent first presentations of immunodeficiency were respiratory tract infections in 63.5% and chronic diarrhea in 17.2%. Common variable immune deficiency (CVID) patients had a higher diagnostic delay than class switching defect (CSD), and agammaglobulinemia. Among the noninfectious complications, autoimmunity (26.2%), and splenomegaly (23.4%) were the most common. Lymphadenopathy was higher in CSD patients than other PADs, while splenomegaly, hepatomegaly, autoimmunity and bronchiectasis were more common in CVID patients than others. Atopic manifestations were mostly recorded in patients with selective IgA deficiency. Malignancy was only reported in 5.8% of patients with CVID. There was a higher prevalence of autoimmune manifestations in CVID comparing to other PADs.

Conclusion: PADs are relatively rare diseases and these patients have a variety of first clinical manifestations, such as diverse infections, autoimmunity, lymphoproliferation, allergy, enteropathy and malignancy. Practitioner’s awareness about the heterogeneous presentations of PAD disorders is poor, therefore patients often are lately diagnosed, and they are complicated with several clinical complications before the certain diagnosis.

 

For more details, please visit: http://www.eurekaselect.com/161253