Progress in the Mechanism and Clinical Application of Cilostazol

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Author(s): Huilei Zheng, Hua Yang, Danping Gong, Lanxian Mai, Xiaoling Qiu, Lidai Chen, Xiaozhou Su, Ruoqi Wei, Zhiyu Zeng*.

Journal Name: Current Topics in Medicinal Chemistry

Abstract:

Cilostazol is a unique platelet inhibitor that has been used clinically for more than 20 years. As a phosphodiesterase type III inhibitor, cilostazol is capable of reversible inhibition of platelet aggregation and vasodilation, has antiproliferative effects, and is widely used in the treatment of peripheral arterial disease, cerebrovascular disease, percutaneous coronary intervention, etc. This article briefly reviews the pharmacological mechanisms and clinical application of cilostazol.

Keywords: Mechanism, Clinical Application , Cilostazol, coronary heart disease, Clopidogrel, perfusion

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DOI: 10.2174/1568026619666191122123855
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The Utility and Efficiency Of Diffusion Tensor Imaging Values to Determine Epidermal Growth Factor Receptor Gene Mutation Status in Brain Metastases From Lung Adenocarcinoma: A Preliminary Study

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Author(s): Mehmet Ali Gultekin*, Hacı Mehmet Turk, Ismail Yurtsever, Bahar Atasoy, Altay Aliyev, Temel Fatih Yilmaz, Alpay Alkan.

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

Abstract:

Background: We aimed to investigate whether there were any diffusion tensor imaging (DTI) value differences in brain metastases (BM) due to lung adenocarcinoma based on the epidermal growth factor receptor (EGFR) gene mutation status.

Material and Methods: 17 patients with 32 solid intracranial metastatic lesions from lung adenocarcinoma were included prospectively. Patients were divided according to the EGFR mutation status as EGFR (+) (group 1, n:8) and EGFR wild type (group 2, n:9). The fractional anisotropy (FA), apparent diffusion coefficient (ADC), normalized ADC (nADC), axial diffusivity (AD), and radial diffusivity (RD) values were measured from the solid component of the metastatic lesions and nADC values were calculated. DTI values were compared between group 1 and group 2. Receiver-operating characteristic analysis was used to obtain cut-off values for the parameters presenting a statistical difference between the EGFR gene mutation positive and wild type group.

Results: There were statistically significant differences in measured ADC, nADC, AD, and RD values between group 1 and group 2. The ADC, nADC, AD, and RD values were significantly lower in group 1. There was no significant difference in FA values between two groups. Analysis by the ROC curve method revealed a cut-off value of ≤721 x 10-6 mm2/s for ADC (Sensitivity=72.7, Specificity=85.7); ≤0.820 for nADC (Sensitivity=72.7, Specificity=90.5), ≤886 for AD (Sensitivity=81.8, Specificity=81.0), and ≤588 for RD (Sensitivity=63.6, Specificity=90.5) in differentiating EGFR mutation (+) group from wild type group.

Conclusion: Combination of the decreased ADC, nADC, AD, and RD values in BM due to lung adenocarcinoma can be important for predicting the EGFR gene mutation status. DTI features of the brain metastases from lung adenocarcinoma may be utilized to provide insight into the EGFR mutation status and guide the clinicians for initiation of targeted therapy.

Keywords: Lung adenocarcinoma, Brain metastases, EGFR, Diffusion tensor imaging, Gene mutation, DTI

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DOI: 10.2174/1573405615666191122122207
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Hollow Zinc Oxide Microflowers for Selective Preconcentration Selenium ions in Nature Water

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Author(s): Ting Huang*, Guanghui Yuan.

Journal Name: Current Analytical Chemistry

Abstract:

Background: Selenium is widely used in a variety of products, thus it can be released into environment from sources such as the discharge of industrial waste water and agricultural runoff.

Objective: The determination of selenium(IV) ion in nature water by atomic fluorescence spectrophotometer(AFS) was established using hollow ZnO microflowers as enriched materials. The hollow ZnO microflowers was prepared by hydrothermal method with polystyrene(PS) microspheres as template.

Method: pH of the selenium(IV) solution will influence the adsorption percent on sorbent.The acidity of adsorption and elution was studied on the different pH of the solution. The adsorption isotherm and adsorption capacity were obtained. Atomic fluorescence spectrophotometer (AFS) was used to the determination of selenium ion. The structure of the hollow ZnO microflowers was characterized by XRD, SEM and TEM.

Results: When the pH is between 6.0-7.0, the adsorption percent of Se(IV) can be as high as 93%. It was found the elution percentage of Se(IV) exceed 96% with 5.0 mL 0.01 mol L-1 NaOH in 10 minutes. The maximum adsorption capacity is 31.5 mg g-1, 31.8 mg g-1 and 32.0 mg g-1at 273K, 333K, 353K respectively.

Conclusion: LOD for Se(IV) detection by enrichment achieved 0.006 μg L-1 with linear range of 0.1-200 μg L-1.The method is applied to analyze samples of nature water and GBW(E)080394, the results are satisfactory.

Keywords: Hollow ZnO microflowers, Selenium(IV), Sorption, Preconcentratio, Selenium , Adsorption

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DOI: 10.2174/1573411015666191122120331
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Antiplatelet Effect of a Pulaimab [Anti-GPIIb/IIIa F(ab)2 Injection] Evaluated by a Population Pharmacokinetic-pharmacodynamic Model

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Author(s): Ya-ou Liu, Zi-ning Wang, Chao-yang Chen, Xian-han Zhuang, Chang-geng Ruan, Ying Zhou, Yi-min Cui*.

Journal Name: Current Drug Metabolism

Abstract:

Background: Cardiovascular disease has one of the highest mortality rates among all the diseases. Platelets play an important role in the pathogenesis of cardiovascular diseases. Platelet membrane glycoprotein GPIIb/IIIa antagonists are the most effective antiplatelet drugs, and pulaimab is one of these. The study aims to promote individual medication of pulaimab [anti-GPIIb/IIIa F(ab)2 injection] by discovering the pharmacological relationship among the dose, concentration, and effects. The goal of this study is to establish a population pharmacokinetic-pharmacodynamic model to evaluate the antiplatelet effect of intravenous pulaimab injection.

Methods: Data were collected from 59 healthy subjects who participated in a Phase-I clinical trial. Plasma concentration was used as the pharmacokinetic index, and platelet aggregation inhibition rate was used as the pharmacodynamic index. The basic pharmacokinetics model was a two-compartment model, whereas the basic pharmacodynamics model was a sigmoid-EMAX model with a direct effect. The covariable model was established by a stepwise method. The final model was verified by a goodness-of-fit method, and predictive performance was assessed by a Bootstrap (BS) method.

Results: In the final model, typical population values of the parameters were as follows: central distribution Volume (V1), 183 L; peripheral distribution Volume (V2), 349 L; Central Clearance (CL), 31 L/h; peripheral clearance(Q), 204 L/h; effect compartment concentration reaching half of the maximum effect (EC50), 0.252 mg/L; maximum effect value (EMAX), 54.0%; and shape factor (γ), 0.42. In the covariable model, thrombin time had significant effects on CL and EMAX. The verification by the goodness-of-fit and BS methods showed that the final model was stable and reliable.

Conclusion: A model was successfully established to evaluate the antiplatelet effect of intravenous pulaimab injection that could provide support for the clinical therapeutic regimen.

Keywords: Chinese Healthy Subjects, Pulaimab [Anti-Gpiib/Iiia F(Ab)2 Injection], Antiplatelet, Population Pharmacokinetics, Population Pharmacodynamics, Model

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DOI: 10.2174/1389200220666191122120238
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Single Channel EEG signal for Automatic Detection of Absence Seizure using Convolutional Neural Network

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Author(s): Niha Kamal Basha*, Aisha Banu Wahab.

Journal Name: Recent Advances in Computer Science and Communications
Formerly: Recent Patents on Computer Science

Abstract:

Absence seizure is a type of brain disorder in which subject get into sudden lapses in attention. Which means sudden change in brain stimulation. Most of this type of disorder is widely found in children’s (5-18 years). These Electroencephalogram (EEG) signals are captured with long term monitoring system and are analyzed individually. In this paper, a Convolutional Neural Network to extract single channel EEG seizure features like Power, log sum of wavelet transform, cross correlation, and mean phase variance of each frame in a windows are extracted after pre-processing and classify them into normal or absence seizure class, is proposed as an empowerment of monitoring system by automatic detection of absence seizure. The training data is collected from the normal and absence seizure subjects in the form of Electroencephalogram. The objective is to perform automatic detection of absence seizure using single channel electroencephalogram signal as input. Here the data is used to train the proposed Convolutional Neural Network to extract and classify absence seizure. The Convolutional Neural Network consist of three layers 1] convolutional layer – which extract the features in the form of vector 2] Pooling layer – the dimensionality of output from convolutional layer is reduced and 3] Fully connected layer–the activation function called soft-max is used to find the probability distribution of output class. This paper goes through the automatic detection of absence seizure in detail and provide the comparative analysis of classification between Support Vector Machine and Convolutional Neural Network. The proposed approach outperforms the performance of Support Vector Machine by 80% in automatic detection of absence seizure and validated using confusion matrix.

Keywords: Absence Seizure Detection, Brain Disorder, Electroencephalogram (EEG), Epilepsy, Feature Extraction, Neural Network, Wavelet Transform

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DOI: 10.2174/2666255813666191122114608
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Molecular Mechanisms Involved in the Antitumor Activity of Isolated Lectins from Marine Organisms: A Systematic Review

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Author(s): Hugo Jefferson Ferreira, Evandro Moreira de Almeida, Wildson Max Barbosa da Silva, Edson Holanda Teixeira, Luiz Gonzaga do Nascimento Neto*.

Journal Name: Current Drug Targets

Abstract:

Introduction: Tumor cells may present several molecular alterations that favor their malignancy, among which there is the expression of tumor-related antigens, such as truncated T-glycans, Thomsen-nouvelle, sialyl-Lewis X and sialyl Tn, which may help in the diagnosis and treatment using specific target molecules. Lectins are ubiquitous proteins capable of interacting with specific carbohydrates. Lectins isolated from marine organisms have important characteristics such as low immunogenicity and can bind to complex glycans compared to plant lectins.

Objective: This work evaluated, through a systematic review, the molecular mechanisms of antitumor activity of lectins isolated from marine organisms. Methodology: The Pubmed, Lilacs, Science Direct, Wiley and Scopus databases were reviewed using the descriptors: marine lectin and cancer. Articles in English, published between January 2008 and December 2018, which proposed the molecular mechanisms of anticancer activity of lectins from marine organisms were eligible for the study.

Results: 17 articles were eligible. The lectins showed promising performance against cancer cells, presenting specific cytotoxicity for some types of malignant cells. The articles presented several lectins specific to different carbohydrates, modulating: pro and anti-apoptotic proteins, transcription factor E2F-1, via mitogen-activated protein kinase. In addition, exogenous lectin expression in cancer cells has been shown to be a promising way to treat cancer.

Conclusion: This review showed the various studies that described the molecular mechanisms caused by marine lectins with antineoplastic potential. This knowledge is relevant for the development and use of the next generations of lectins isolated from marine organisms, supporting their potential in cancer treatment.

Keywords: Cancer, Marine lectin, Antineoplastic, Natural Product, Molecular mechanisms, Marine organisms

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DOI: 10.2174/1389450120666191122113850
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An Anatomy of a Hybrid Color Descriptor with a Neural Network Model to Enhance the Retrieval Accuracy of an Image Retrieval System

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Author(s): Shikha Bhardwaj*, Gitanjali Pandove, Pawan Kumar Dahiya.

Journal Name: Recent Advances in Computer Science and Communications
Formerly: Recent Patents on Computer Science

Abstract:

Background: In order to retrieve a particular image from vast repository of images, an efficient system is required and such an eminent system is well-known by the name Content-based image retrieval (CBIR) system. Color is indeed an important attribute of an image and the proposed system consist of a hybrid color descriptor which is used for color feature extraction. Deep learning, has gained a prominent importance in the current era. So, the performance of this fusion based color descriptor is also analyzed in the presence of Deep learning classifiers.

Method: This paper describes a comparative experimental analysis on various color descriptors and the best two are chosen to form an efficient color based hybrid system denoted as combined color moment-color autocorrelogram (Co-CMCAC). Then, to increase the retrieval accuracy of the hybrid system, a Cascade forward back propagation neural network (CFBPNN) is used. The classification accuracy obtained by using CFBPNN is also compared to Patternnet neural network.

Results: The results of the hybrid color descriptor depict that the proposed system has superior results of the order of 95.4%, 88.2%, 84.4% and 96.05% on Corel-1K, Corel-5K, Corel-10K and Oxford flower benchmark datasets respectively as compared to many state-of-the-art related techniques.

Conclusion: This paper depict an experimental and analytical analysis on different color feature descriptors namely, Color moment (CM), Color auto-correlogram (CAC), Color histogram (CH), Color coherence vector (CCV) and Dominant color descriptor (DCD). The proposed hybrid color descriptor (Co-CMCAC) is utilized for the withdrawal of color features with Cascade forward back propagation neural network (CFBPNN) is used as a classifier on four benchmark datasets namely Corel-1K, Corel-5K and Corel-10K and Oxford flower.

Keywords: Color Moment, Color Auto-Correlogram, Color Histogram, Dominant Color Descriptor, Color Coherence Vector, Cascade Forward Neural Network, Patternnet Neural Network

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DOI: 10.2174/2666255813666191122113801
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Design and synthesis of 4(1H)-quinolone derivatives as autophagy inducing agents by targeting ATG5 protein

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Author(s): Yifan Jia, Difei Yu, Qiuhua Huang, Xiaodong Zhang, Liqin Qiu, Rihui Cao*, Runlei Du, Wenbin Liu.

Journal Name: Letters in Drug Design & Discovery

Abstract:

Background: Quinolines have been characterized as a class of potential antitumor agents, and a large number of natural and synthetic quinolines acting as antitumor agents were reported.

Methods: A series of 7-chloro-4(1H)-quinolone derivatives were synthesized. Antiproliferative effect of these compounds was evaluated by MTT assay against five human tumor cell lines. The mechanism of action of the selected compound 7h was investigated.

Results and Discussion: Most of the compounds had more potent antiproliferative activities than the lead compound 7-chloro-4(1H)-quinolone 6b. Compound 7h was found to be the most potent antiproliferative agent against human tumor cell lines. Further investigation demonstrated that compound 7h triggered ATG5-dependent autophagy of colorectal cancer cells by promoting the functions of LC3 proteins.

Conclusion: These results were useful for designing and discovering more potent novel antitumor agents endowed with better pharmacological profiles.

Keywords: Synthesis, Quinolone, Antiproliferative, Autophagy, Mechanism Of Action, ATG5 Protein

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DOI: 10.2174/1570180816666191122113045
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Organo- or metal complex catalyzed synthesis of five-membered oxygen heterocycles

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Author(s): Navjeet Kaur*, Neha Ahlawat, Pooja Grewal, Pranshu Bhardwaj, Yamini Verma.

Journal Name: Current Organic Chemistry

Abstract:

The reactions involving formation of C-O bond using metal as a catalyst have emerged to be one of the most influential reactions for the synthesis of the heterocycles in modern organic chemistry. Catalysis by metals offers diverse opportunity to invent new organic reactions with promising range of selectivities such as chemoselectivity, regioselectivity, diastereoselectivity, and enantioselectivity. The methodologies used earlier for synthesis were less approachable to the organic chemist because of their high cost, highly specified instrumentation and inconvenient methods. For both stereoselective and regioselective formation of five-membered O-containing heterocycles, cyclic reactions that are metal and non-metal-catalyzed have known to be very efficient. The present review article covers the applications of metal and non-metal as a catalyst for the synthesis of five-membered O-containing heterocycles.

Keywords: Catalysis, Heterocycles, Oxygen, Furans, Dioxolanes, Synthesis

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DOI: 10.2174/1385272823666191122111351
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