Most Accessed Articles | Assessment of Auditory Pathways Using Diffusion Tensor Imaging in Patients with Neurofibromatosis Type 1

Journal Name: Current Medical Imaging
Formerly: Current Medical Imaging Reviews

 

 

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Aim: The aim of our study was to determine whether the diffusion properties of the auditory pathways alter between patients with Neurofibromatosis type 1 (NF1) and the healthy subjects. DTI can well demonstrate FA and ADC changes in auditory tracts and it may be a guide to identify the candidates for hearing loss among NF1 children.

Methods: The study population consisted of 43 patients with NF1 and 21 healthy controls. Diffusion tensor imaging (DTI) was used to measure apparent diffusion coefficient (ADC) and fractional anisotropy (FA) values from lemniscus lateralis, colliculus inferior, corpus geniculatum mediale and Heschl’s gyrus. The results were compared with those of the control group.

Results: The ADC values of lateral lemniscus, colliculus inferior and corpus geniculatum mediale were significantly higher in NF1 compared to those of the control group. On the other hand, decreased FA values were observed in lateral lemniscus and colliculus inferior in patients with NF1.

Conclusion: The increase in ADC and reduction in FA in the auditory pathways of patients with NF1 may suggest microstructural alterations, such as a decrease in the number of axons, edema or inflammation in the auditory tracts. To read out more, please visit: http://www.eurekaselect.com/161550/article

Most Accessed Articles | Identification of New Inhibitors of Mutant Isocitrate Dehydrogenase 2 through Molecular Similarity-based Virtual Screening

Journal Name: Letters in Drug Design & Discovery

Author(s): Lijun Yang, Stefan Pusch, Victoria Jennings, Tianfang Ma, Qihua Zhu, Yungen Xu, Andreas von Deimling*, Xiaoming Zha*.

 

 

 

 

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Background: Isocitrate dehydrogenase 2 (IDH2) is an enzyme catalyzing the oxidative decarboxylation of isocitrate to α-ketoglutarate (α-KG) in the tricarboxylic acid (TCA). Evidences suggest that the specific mutations in IDH2 are critical to the growth and reproduction of severe tumors especially leukemia and glioblastoma. It is found that the inhibitors of mutant IDH2 are promising anti-tumor therapeutics.

Methods: A virtual screening strategy combining molecular similarity search and molecular docking was performed in the binding site of AGI-6780. YL-16, YL-17 and YL-18 were identified as novel mutant IDH2 inhibitors for the reduction of (D)-2-hydroxyglutarate in cellular evaluation. In addition, all the three compounds showed inhibition against IDH2-R172K mutated HEK-293T cells, while weak inhibition against wide-type IDH2 (WT-IDH2) HEK-293T cells.

Results: Significantly, YL-17 showed 84.55% inhibitory activity against IDH2-R172K at 1 µM and weak cytotoxicity to wide-type IDH2 at 50 µM.

Conclusion: YL-17 was highlighted as a new mutant IDH2 inhibitor that could be further developed for therapeutic applications. To read out more, please visit: http://www.eurekaselect.com/164444/article

Most Accessed Articles | Development of an HPLC-UV Method for Quantification of Stattic

Journal Name: Current Pharmaceutical Analysis

Author(s): Soheil Sedaghat, Ommoleila Molavi, Akram Faridi, Ali Shayanfar*, Mohammad Reza Rashidi.

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Background: Signal transducer and activator of transcription 3 (STAT3), an oncogenic protein found constitutively active in many types of human malignancies, is considered to be a promising target for cancer therapy.

Objective: In this study for the first time, a simple and accurate method has been developed for the determination of a STAT3 dimerization inhibitor called stattic in aqueous and plasma samples.

Methods: A reverse-phase high-performance liquid chromatography (RP-HPLC) composed of C18 column as stationary phase, and the mixture of acetonitrile (60%) and water (40%) as mobile phase with a UV detection at 215 nm were applied for quantification of stattic. The developed method was validated by Food and Drug Administration (FDA) guideline.

Results: The method provided a linear range between 1-40 and 2.5-40 µg mL-1 for aqueous and plasma samples, respectively, with a correlation coefficient of 0.999. The accuracy (as recovery) of the developed method was found to be between 95-105% for aqueous medium and 85-115% for plasma samples. The precision (as relative standard deviation) for aqueous and plasma samples was less than 6% and 15%, respectively. The sensitivity of the developed method based on FDA guideline was 1 µg mL-1 for aqueous and 2.5 µg mL-1 for plasma samples.

Conclusion: These results show that the established method is a fast and accurate quantification for stattic in aqueous and plasma samples. To read out more, please visit: http://www.eurekaselect.com/162366/article

Most Accessed Articles | QSAR Analysis of Multimodal Antidepressants Vortioxetine Analogs Using Physicochemical Descriptors and MLR Modeling

Journal Name: Current Computer-Aided Drug Design

Author(s): David M. Rajathei*, Subbiah Parthasarathy, Samuel Selvaraj.

 

 

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Background: Vortioxetine is a multimodal antidepressant drug with combined effects on SERT as an inhibitor, 5-HT1A as agonist and 5-HT3A as an antagonist. Series of vortioxetine analogs have been reported as multi antidepressant compounds and they block serotonin transport into the neuronal cells, activate the postsynaptic 5-HT1A receptors and eliminate the low activity of 5-HT3A receptors.

Objective: To explore the important properties of vortioxetine analogs involved in antidepressant activity by developing 2D QSAR models.

Methods: Selections of significant descriptors were performed by Least Absolute Shrinkage and Selection Operator (LASSO) method and, the Multiple Linear Regression (MLR) method and All Subsets and GA algorithm included in QSARINS software were used for generating QSAR models. Further, the virtual screening was performed based on bioactivity and structure similarity using the PubChem database.

Results: The four descriptor model of complementary information content (CIC2), solubility (bcutp3), mass (bcutm8) and partial charge in van der Waals surface area (PEOEVSA7) of the molecules is obtained for SERT inhibition with the significant statistics of R2= 0.69, RMSEtr= 0.44, R2 ext= 0.62 and CCCext= 0.78. For 5-HT1A agonist, the two descriptor model of molecular shape (Kappm3) and van der Waals volume of the atoms (bcutv11) with R2= 0.78, RMSEtr= 0.33, R2 ext = 0.83, and CCCext= 0.87 is established. The three descriptor model of information content (IC3), solubility (bcutp9) and electronegativity (GATSe5) of the molecules with R2= 0.61, RMSEtr= 0.34, R2 ext= 0.69 and CCCext= 0.72 is obtained for 5-HT3A antagonist. The antidepressant activities of 16 virtual screened compounds were predicted using the developed models.

Conclusion: The developed QSAR models may be useful to predict antidepressant activity for the newly synthesized vortioxetine analogs. To read out more, please visit: http://www.eurekaselect.com/166166/article

Most Accessed Articles | Molecular Diagnosis of Fibro-osseous Lesions of the Oral and Maxillofacial Region: A Tale from Africa

Journal Name: Current Dentistry

Author(s): Olujide O. Soyele, Adeyinka H. Adedapo, Henry A. Adeola*.

 

 

Fibro-osseous lesions (FOLs) are a poorly defined but pathologically diverse group of lesions affecting the craniofacial bones and jaw. They are mostly characterized by the replacement of bone by a benign connective tissue matrix, which may contain foci of mineralization in the form of woven bone or cementum-like round acellular intensely basophilic structures. These lesions, although diverse, often present similar clinico-pathological and radiographic features. This often leads to difficulty in diagnosis and management. Definitive diagnosis is often reached only by incisional or excisional biopsy in resource-limited settings. Epidemiologically, the incidence and prevalence of different FOLs have been variable depending on the region. Reports from Africa indicated that FOLs make up to 10% of all oral biopsies, while others have given lower figures. A good understanding of the pathogenetic mechanism for FOLs is important, and state of the art molecular approaches are bound to improve the diagnosis and delineation of various entities that fall under the FOL category. Not least, the classification and nomenclature of these lesions by the World Health Organization (WHO) have changed significantly over the years. Hence, we have presented in this review a robust discussion on the pathobiology, emerging molecular markers, diagnostic challenges, future perspectives and recent changes to the classification/nomenclature of FOLs by WHO. In addition, we also discussed the diagnostic bottlenecks encountered during diagnosis of FOL in Africa. To read out more, please visit: http://www.eurekaselect.com/163030/article

Most Accessed Articles | Antibacterial Profile of Copaifera multijuga Oleoresin and Hydroalcoholic Extract of Leaves Against Oral Pathogens

 

Journal Name: Current Dentistry

Author(s): Iane Pereira Pimenta, Fariza Abrão, Jonas Joaquim Mangabeira da Silva, Larissa Costa Oliveira, Hervé Louis Ghislain Rogez, Sérgio Ricardo Ambrósio, Rodrigo Cássio Sola Veneziani, Jairo Kenupp Bastos, Carlos Henrique Gomes Martins*.

 

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Background: Copaifera multijuga are widely used as medicinal plants in Brazil. Of the various ethnopharmacological indications of copaiba oleoresins, the antimicrobial activity had been highlighted.

Objective: This study aimed to evaluate the oleoresin and the hydroalcoholic extract of leaves from Copaifera multijuga against oral pathogens in the sessile and in the planktonic modes.

Methods: Standard strains from the American Type Culture Collection and clinical isolates which cause both cariogenic and endodontic infections were used. Was evaluated in terms of its Minimum Inhibitory Concentration (MIC) values by the broth microdilution method in 96-well microplates, Minimum Bactericidal Concentration (MBC) and biofilm eradication assay.

Results: The Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) assays showed that the oleoresin was effective against some the bacterial strains. Assessment of the antibiofilm activity of hydroalcoholic extract of leaves from C. multijuga against the evaluated microaerophilic bacteria in the sessile mode gave IC50 values of 318.0 and 695.6 µg/mL against S. mitis (ATCC 49456) and A. actinomycetemcomintans (ATCC 43717), respectively. As for the assayed anaerobic bacteria, the hydroalcoholic extract of leaves gave IC50 of 4554.0, 2218.0, and 600.1 µg/mL against F. nucleatum (Clinical isolate), P. gingivalis (ATCC 33277), and P. micros (Clinical isolate), respectively, whereas the oleoresin afforded IC50 of 357.1 µg/mL against P. gingivalis (ATCC 33277).

Conclusion: The oleoresin and hydroalcoholic extract of leaves displayed satisfactory activity against the main oral pathogens in both sessile and planktonic modes. The oleoresin and hydroalcoholic extracts of leaves from C. multijuga are potential candidates for the development of new products for dental and oral care. To read out more, please visit: http://www.eurekaselect.com/163330/article

Most Accessed Articles| Stroke Lesion Segmentation and Analysis using Entropy/Otsu’s Function – A Study with Social Group Optimization

Journal Name: Current Bioinformatics

Author(s): Suresh Chandra Satapathy*, Steven Lawrence Fernandes, Hong Lin.

 

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Background: Stroke is one of the major causes for the momentary/permanent disability in the human community. Usually, stroke will originate in the brain section because of the neurological deficit and this kind of brain abnormality can be predicted by scrutinizing the periphery of brain region. Magnetic Resonance Image (MRI) is the extensively considered imaging procedure to record the interior sections of the brain to support visual inspection process.

Objective: In the proposed work, a semi-automated examination procedure is proposed to inspect the province and the severity of the stroke lesion using the MRI.

Method: Recently discovered heuristic approach called the Social Group Optimization (SGO) algorithm is considered to pre-process the test image based on a chosen image multi-thresholding procedure. Later, a chosen segmentation procedure is considered in the post-processing section to mine the stroke lesion from the pre-processed image.

Results: In this paper, the pre-processing work is executed with the well known thresholding approaches, such as Shannon’s entropy, Kapur’s entropy and Otsu’s function. Similarly, the postprocessing task is executed using most successful procedures, such as level set, active contour and watershed algorithm.

Conclusion: The proposed procedure is experimentally inspected using the benchmark brain stroke database known as Ischemic Stroke Lesion Segmentation (ISLES 2015) challenge database. The results of this experimental work authenticates that, Shannon’s approach along with the LS segmentation offers superior average values compared with the other approaches considered in this research work. To read out more, please visit: http://www.eurekaselect.com/168477

Most Accessed Articles | Dysfunctional Mechanism of Liver Cancer Mediated by Transcription Factor and Non-coding RNA

Journal Name: Current Bioinformatics

Author(s): Wei Zeng, Fang Wang, Yu Ma, Xianchun Liang, Ping Chen*.

 

 

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Background: There have been numerous experiments and studies on liver cancer by biomedical scientists, while no comprehensive and systematic exploration has yet been conducted. Therefore, this study aimed to systematically dissect the transcriptional and non-coding RNAmediated mechanisms of liver cancer dysfunction.

Method: At first, we collected 974 liver cancer associated genes from the Online Mendelian Inheritance in Man (OMIM). Afterwards, their interactors were recruited from STRING database so as to identify 18 co-expression modules in liver cancer patient expression profile. Crosstalk analysis showed the interactive relationship between these modules. In addition, core drivers for modules were identified, including 111 transcription factors (STAT3, JUN and NFKB1, etc.) and 1492 ncRNAs (FENDRR and miR-340-5p, etc.) Read out full article here: http://www.eurekaselect.com/167479

Most Accessed Articles | Structural Barriers to Pre-exposure Prophylaxis Use Among Young Sexual Minority Men: The P18 Cohort Study

Journal Name: Current HIV Research

Author(s): Jessica Jaiswal*, Marybec Griffin, Stuart N. Singer, Richard E. Greene, Ingrid Lizette Zambrano Acosta, Saara K. Kaudeyr, Farzana Kapadia, Perry N. Halkitis.

 

 

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Background: Despite decreasing rates of HIV among many populations, HIV-related health disparities among gay, bisexual and other men who have sex with men persist, with disproportional percentages of new HIV diagnoses among racial and ethnic minority men. Despite increasing awareness of HIV pre-exposure prophylaxis (PrEP), PrEP use remains low. In addition to exploring individual-level factors for this slow uptake, structural drivers of PrEP use must also be identified in order to maximize the effectiveness of biomedical HIV prevention strategies.

Method: Using cross-sectional data from an ongoing cohort study of young sexual minority men (N=492), we examine the extent to which structural-level barriers, including access to health care, medication logistics, counseling support, and stigma are related to PrEP use.

Results: While almost all participants indicated awareness of PrEP, only 14% had ever used PrEP. PrEP use was associated with lower concerns about health care access, particularly paying for PrEP. Those with greater concerns talking with their provider about their sexual behaviors were less likely to use PrEP.

Conclusion: Paying for PrEP and talking to one’s provider about sexual behaviors are concerns for young sexual minority men. In particular, stigma from healthcare providers poses a significant barrier to PrEP use in this population. Providers need not only to increase their own awareness of and advocacy for PrEP as an effective risk-management strategy for HIV prevention, but also must work to create open and non-judgmental spaces in which patients can discuss sexual behaviors without the fear of stigma.

 

Read out more at: http://www.eurekaselect.com/164166 

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