Evaluation of insulin resistance induced brain tissue dysfunction in obese dams and their neonates: Role of ipriflavone amelioration

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Author(s): Rania A. Gad, Eman S. Abdel-Reheim, Gaber M.G. Shehab, Hani S. Hafez, Abdelaziz S.A. Abuelsaad*

Journal Name: Combinatorial Chemistry & High Throughput Screening
Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry and Natural Products Research

Abstract:

Background: Nonalcoholic steatohepatitis (NASH) is associated with activation of liver fibrogenesis and predisposes to cirrhosis and associated morbi-mortality. A high fat high cholesterol diet (HFD) was provided to female albino rats to establish a NASH model. It is well known that the offspring of obese mothers have an increased risk of obesity and diabetes. The present study aimed at evaluating the ameliorative effects of ipriflavone (IP) as a natural food supplement on the lipid metabolism, improving insulin sensitivity, reducing oxidative stress and inflammation, modifying metabolic risk factors and/or reduce brain damage, in both neonates and their dams.

Materials and Methods: The present aim was achieved by evaluating the oxidative stress and antioxidant defense system biomarkers, as thiobarbituric acid reactive substances (TBARS) and reduced glutathione (GSH), catalase, and superoxide dismutase (SOD) activities. In addition, neurotransmitter acetylcholine (Ach) and acetylcholine esterase (AchE) activities, as well as levels of the apolipoprotein E4 (APOE4); β-secretase, hyper phosphor-tau and β-amyloid 42; 3-hydroxy-3-methyl glutaryl coenzyme A reductase (HMG CoA R)” and COX-II by immunoblotting assays in the brain tissue of neonates and theirs dams in all the studied groups.

Results: A very significant amelioration in acetylcholine and acetylcholine esterase neurotransmitters, Alzheimer’s makers (β-amyloid), antioxidants (reduced glutathione (GSH) contents, catalase (CAT) and superoxide dismutase (SOD); and inflammatory cytokines in NASH model is observed upon administrating ipriflavone (IP) as a natural food supplement. The multifunctional activities of ipriflavone as an antioxidant, anti-inflammatory and anti-insulin resistance drug were discussed and correlated with other investigations.

Conclusion: Regarding steatohepatitis, the present study confirmed the anti-inflammatory effects of the ipriflavone (IP). Therefore, future studies should focus on hepatic fatty acid uptake, hepatic lipogenesis, and fatty acid oxidation and the role of IP in regulating hepatic fat metabolism. In addition, natural products like IP could be combined with the highly used pharmaceutical drugs to reduce the side effects of nonalcoholic steatohepatitis, and minimize progression of dementia. Moreover, present study supports further attempts to heal the neural dysfunction via antioxidant and anti-inflammatory cascade activities using ipriflavone (IP).

Keywords: Neonates - Obesity - insulin resistance - Nonalcoholic fatty liver disease (NAFLD)”- Ipriflavone - HMG CoA R- Acetylcholine esterase - β_Secretase – APOE4- Oxidative stress.

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DOI: 10.2174/1386207323666200808181148
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Nickel(II) Chromite Nanoparticles: An Eco-Friendly and Reusable Catalyst for Synthesis of 2,4-Diamino-6-aryl-pyrimidine-5-yl Cyanides under Ultrasonic Radiation

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Author(s): Bahareh Saeedi, Shahrzad Abdolmohammadi*, Zohreh Mirjafary, Reza Kia-Kojoori

Journal Name: Combinatorial Chemistry & High Throughput Screening
Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry and Natural Products Research

Abstract:

Background: One of the principal factors in the field of research in green chemistry is to drive chemical reactions under ultrasonication as a versatile synthetic tool. Moreover, nanostructured metal salts occupy an important position as low cost, efficient, heterogeneous, and green catalysts in chemical reactions. Pyrimidine has also acquired significance because it is a core structure in a variety of natural and non-natural agents, many of which display versatile biological activities and medical applications.

Objective: The aim of this study was to explore the role of nickel(II) chromite nanoparticles (NiCr2O4 NPs) as a green and recyclable catalyst for the synthesis of 2,4-diamino-6-aryl-pyrimidine-5-yl cyanides under ultrasonic radiation.

Methods: A direct cyclocondensation reaction of guanidine nitrate, aromatic aldehydes, and malononitrile were performed using NiCr2O4 NPs as an effective heterogeneous catalyst under ultrasonic radiation at room temperature conditions to prepare 2,4-diamino-6-aryl-pyrimidine-5-yl cyanides in high yields. The described catalyst was prepared successfully according to a simple hydrothermal route and fully characterized by the X-Ray diffraction (XRD) technique, energy dispersive X-Ray (EDS) analysis, scanning electron microscopy (SEM), and dynamic light scattering (DLS).

Results: A number of 2,4-diamino-6-aryl-pyrimidine-5-yl cyanides were effectively synthesized in high yields (94-98%) within short reaction times (15 min). All synthesized compounds were well characterized by IR, 1H and 13C NMR spectroscopy, and also by elemental analyses.

Conclusion: In conclusion, a simple, efficient, and green synthesis of 2,4-diamino-6-aryl-pyrimidine-5-yl cyanides was developed using NiCr2O4 NPs as green nanocatalyst, and under ultrasound radiation as green tool. The mild reaction conditions, avoiding the use of toxic solvents or reagents, high atom economy, high yields, and simple work-up are the attractive features of this new protocol.

Keywords: Green synthesis, nickel(II) chromite nanoparticles (NiCr2O4 NPs), pyrimidines, recyclability of catalyst, ultrasonic radiation.

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DOI: 10.2174/1386207323666200808180527
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Acknowledgements to Reviewers

Author(s):

Journal Name: Current Vascular Pharmacology

Volume 18 , Issue 6 , 2020

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VOLUME: 18
ISSUE: 6
Year: 2020
Page: [667 - 667]
Pages: 1
DOI: 10.2174/157016111806200808180120





Variations in Mineral/heavy metals profiling and preventive role of trichomes in Peach Fruits treated with CaC2

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Author(s): Muhammad Irfan, Safdar Abbas, Beenish Jehan Azhar, Shakeel Ahmad, Hafsa Muhammad*, Ishaq Ahmed, Javed Hussain, Samina N Shakeel

Journal Name: Combinatorial Chemistry & High Throughput Screening
Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry and Natural Products Research

Abstract:

Background: Phytonutrients in peach fruits have health promoting antioxidants against various chronic diseases. However, there is no extensive data to show the nutritional values of Local peach cultivars after post-harvest treatments.

Objective: Mainly this study was objective to determine the effect of calcium carbide on nutritional value and quality of fruits of Pakistani peach cultivars.

Methods: The peach fruits were collected from three different peach orchids of KPK and the fruits were divided into 4 groups while 5th group was collected from local fruit shop. Each experimental group was treated with different concentration of calcium carbide whereas control group was not treated. The peel and pulp samples were oven dried and ground to fine powder separately. The elemental compositions were determined using Particle Induced X-ray emission and Pelletron Tandem Accelerator.

Result: Sixteen elements were identified in peach fruits and the elements were Al, P, S, Cl, K, Ca, Cr, Mn, Fe, Co, Ni, Cu, Zn, As, and Se. In peel, concentration of some elements increased or decreased after treatment with CaC2 while in pulp the conc. of nearly all detected elements was increased in treated samples. We found significantly high amount of heavy metals traces including As, Se, Co, Si, and P in peach fruits treated with CaC2. Interestingly, the presence of trichomes in peach skin prevents the transfer of these heavy metals deep into the pulp which was also verified by the elemental profiling of nectarines.

Conclusion: Conclusively, the artificial ripening with CaC2 changed the nutritional value of peach fruits that has higher health risks if consume with the peel. According to our best knowledge, this is the first report that highlights the effects of CaC2 which deteriorate the nutritional value of peach fruits in Pakistan.

Keywords: Phytonutrients, Minerals, Fruits, Peach, Artificial ripening, Calcium carbide

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DOI: 10.2174/1386207323666200808175723
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Transcriptome-wide association study identifies genetically dysregulated genes in diabetic neuropathy

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Author(s): Danfeng Lan, Hong-Yan Jiang, Xiaoyang Su, Yan Zhao, Sicheng Du, Ying Li, Rui Bi, Deng-Feng Zhang, Qiuping Yang*

Journal Name: Combinatorial Chemistry & High Throughput Screening
Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry and Natural Products Research

Abstract:

Background: Complications are the main cause of the disease burden of diabetes. Genes determining the development and progression of complications remain to be identified. Diabetic neuropathy is the most common and debilitating complication and mainly affects the nerves of legs and feet. In this study, we attempted to identify diabetic neuropathy-specific genes from reliable large-scale genome-wide association studies (GWASs) for diabetes per se.

Methods: Taking advantage of publicly available data, we initially converted the GWAS signals to transcriptomic profiles in the tibial nerve using the functional summary-based imputation (FUSION) algorithm. The FUSION-derived genes were then checked to determine whether they were differentially expressed in the sciatic nerve of mouse models of diabetic neuropathy. The dysregulated genes identified in the sciatic nerve were explored in the blood of patients.

Results: We found that eleven genes out of 452 FUSION-derived genes were regulated by diabetes GWAS loci and were altered in the sciatic nerve of mouse models with early-stage neuropathy. Among the eleven genes, significant (Pvalue<0.05) expression alterations of HSD17B4, DHX32, MERTK, and SFXN4 could be detected in the blood of human patients.

Conclusions: Our analyses identified genes with an effect in the sciatic nerve and provided the possibility of noninvasive early detection of diabetic neuropathy.

Keywords: Diabetic neuropathy, genome-wide association study, transcriptome-wide association study, differential expression, expression quantitative trait loci.

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DOI: 10.2174/1386207323666200808173745
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Screening of Hub Gene Targets for Lung Cancer via Microarray Data

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Author(s): Chang Su*, Wen-Xiu Liu, Li-Sha Wu, Tian-Jian Dong, Jun-Feng Liu

Journal Name: Combinatorial Chemistry & High Throughput Screening
Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry and Natural Products Research

Abstract:

Background: Lung cancer is one of the malignancies exhibiting the fastest increase in morbidity and mortality, but the cause is not clearly understood. The goal of this investigation was to screen and identify relevant biomarkers of lung cancer.

Methods: Publicly available lung cancer data sets, including GSE40275 and GSE134381, were obtained from the GEO database. The repeatability test for data was done by principal component analysis (PCA), and a GEO2R was performed to screen differentially expressed genes (DEGs), which were all subjected to enrichment analysis. Protein-protein interactions (PPIs), and the significant module and hub genes were identified via Cytoscape. Expression and correlation analysis of hub genes was done, and an overall survival analysis of lung cancer was performed. A receiver operating characteristic (ROC) curve analysis was performed to test the sensitivity and specificity of the identified hub genes for diagnosing lung cancer.

Results: The repeatability of the two datasets was good and 115 DEGs and 10 hub genes were identified. Functional analysis revealed that these DEGs were associated with cell adhesion, the extracellular matrix, and calcium ion binding. The DEGs were mainly involved with ECM-receptor interaction, ABC transporters, cell-adhesion molecules, and the p53 signaling pathway. Ten genes including COL1A2, POSTN, DSG2, CDKN2A, COL1A1, KRT19, SLC2A1, SERPINB5, DSC3, and SPP1 were identified as hub genes through module analysis in the PPI network. Lung cancer patients with high expression of COL1A2, POSTN, DSG2, CDKN2A, COL1A1, SLC2A1, SERPINB5, and SPP1 had poorer overall survival times than those with low expression (p <0.05). The CTD database showed that 10 hub genes were closely related to lung cancer. Expression of POSTN, DSG2, CDKN2A, COL1A1, SLC2A1, SERPINB5, and SPP1 was also associated with a diagnosis of lung cancer (p<0.05). ROC analysis showed that SPP1 (AUC = 0.940, p = 0.000*, 95%CI = 0.930-0.973, ODT = 7.004), SLC2A1 (AUC = 0.889, p = 0.000*, 95%CI = 0.791-0.865, ODT = 7.123), CDKN2A (AUC = 0.730, p = 0.000*, 95%CI = 0.465-1.000, ODT = 6.071) were suitable biomarkers.

Conclusions: Microarray technology represents an effective method for exploring genetic targets and molecular mechanisms of lung cancer. In addition, identification of hub genes of lung cancer provides novel research insights for the diagnosis and treatment of lung cancer.

Keywords: lung cancer, hub gene, differentially expressed genes, bioinformatics, overall survival

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DOI: 10.2174/1386207323666200808172631
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Exploration of the Potential Mechanism of Calculus Bovis in Treatment of Primary Liver Cancer by Network Pharmacology

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Author(s): Zhen Zhang*, Puhua Zeng, Wenhui Gao, Ruoxia Wu, Tianhao Deng, Siqin Chen, Xuefei Tian

Journal Name: Combinatorial Chemistry & High Throughput Screening
Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry and Natural Products Research

Abstract:

Aim and Objective: Calculus Bovis (CB) has been employed to treat diseases for a long time. It has been identified to play significant anti-inflammatory and anti-tumor roles. However, the mechanism of treating primary liver cancer (PLC) remains to be revealed. This study aims to clarify the molecules and mechanisms of CB in treating PLC.

Materials and Methods: After oral bioavailability (OB) and drug-likeness (DL) screening, 15 small molecules were identified as the potential ingredients against PLC. Following this, related targets network constructions and pathways were applied to clarify the mechanism of CB in treating PLC. An in vitro experiment was carried out to identify the function of CB in treating PLC.

Results: Eleven compounds of CB were identified that play an anti-PLC role, including oleanolic acid, ergosterol, ursolic acid, etc. The potential targets which were observed include: IL6, MAPK-8, VEGFA, Caspase-3, etc. Further analysis showed that the mechanism of CB in the treatment of PLC involved apoptosis-related pathways and immune- related pathways.

Conclusion: In summary, the current study combines network pharmacology and in vitro experiments to reveal the mechanism of CB against PLC. We concluded that 11 ingredients of CB have an anti-PLC effect. Furthermore, CB plays a key role in treating PLC mainly by apoptosis-related pathways and immune-related pathways. Our experiment verifies that CB promotes the apoptosis of SMMC-7721.

Keywords: Network Pharmacology, Calculus Bovis, Primary Liver Cancer

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DOI: 10.2174/1386207323666200808172051
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Regulatory requirements and comparison in approval of new and generic drugs in United States of America and Japan:-Implication for Future strategies

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Author(s): Paramjeet Malik, Neelam Pawar*, Kavita Bahmani

Journal Name: Applied Clinical Research, Clinical Trials and Regulatory Affairs

Abstract:

Safety, efficacy and quality of a therapeutic product is the major concern for the pharmaceutical companies. FDA and PMDA are the main regulatory authorities in USA & JAPAN respectively that ensures the maintenance of these required parameters by forming standard guidelines and process for drug approval. These regulatory authorities’ reviews each step of a pharmaceutical drug product from its discovery phase to marketed product. Dossier plays an important role during the approval process of a drug product, as it allows both applicant and review team members to evaluate the data in an effective manner. A dossier consists of five modules containing informative data of various stages of a drug product but in a brief pattern with folders and subfolders. In the present paper, the authors focus on in-depth review of approval process for new and generic drugs in USA and Japan.

Keywords: Regulatory, approval, generic drugs, United States of America, Japan

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DOI: 10.2174/2213476X07666200808163247
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A systematic review of traditionally used herbs and animal-derived products as potential analgesics

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Author(s): Kannan RR Rengasamy, Mohamad Fawzi Mahomoodally*, Teshika Joaheer, Yansheng Zhang

Journal Name: Current Neuropharmacology

Abstract:

Pain is a distressing but fundamental manifestation that prepares the body for potentially detrimental stimuli while ensuring its protection. Plant and animal products have traditionally been used to relieve pain for centuries. However, no attempt has been made to compile a single report of plant and animal products possessing analgesic properties. This review enadeavours to recover data from published articles to establish a collective literature review on folk remedies from plant and animal sources used as analgesics and in the treatment of pain-related conditions, identifying gaps in existing knowledge and future works. Relevant information was systematically retrieved using the PRISMA method. In this review, in total, 209 plants were found to be either used raw or prepared by decoctions or maceration. Administration was either oral or topical, and they were predominantly used in Asian countries. In vivo studies of plants with analgesic properties, which were tested using different methods including acetic-induced writhing test, hotplate test, tail-flick test, and formalin-induced pain test, were compiled. Animal products with analgesic properties were obtained mainly from compounds present in venom; their bioactive compounds were also identified. In the literature search, certain gaps were noted, which could be reviewed in future studies. For instance, there was a disparity of information regarding the traditional uses of medicinal plants. In this review, an attempt was made to critically assess and describe the pharmacological properties and bioactive composition of indigenous plants, some animal species, and animal venom by scrutinizing databases and looking for published articles. Therefore, it can be concluded that the compounds obtained from these sources can serve as important ingredients in therapeutic agents to alleviate pain once their limitations are assessed and improved upon. In the literature search, certain gaps were noted, which could be reviewed in future studies.

Keywords: traditional medicine, pain, analgesics, pharmacological, plants, animals

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DOI: 10.2174/1570159X18666200808151522
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Current Vascular Pharmacology

Editor-in-Chief:

Dimitri P. Mikhailidis  
Academic Head, Department of Clinical Biochemistry
Royal Free Hospital Campus
University College London Medical School
University College London (UCL)
Pond Street, London, NW3 2QG
UK

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Antonis S. Manolis* and Athanasios G. Tzioufas
DOI: 10.2174/1570161118666200721145718

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Cardiovascular Disease in Antiphospholipid Syndrome

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Kali Polytarchou*, Dimitrios Varvarousis and Antonis S. Manolis
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Cardiovascular Consequences of Autoimmune Rheumatic Diseases

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Fabiola Atzeni*, Valeria Nucera, Elisabetta Gerratana, Alessia Fiorenza, Luigi Gianturco, Marco Corda and Piercarlo Sarzi-Puttini
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Cardiovascular Disease in Juvenile Idiopathic Arthritis

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Elisavet Arsenaki, Panagiotis Georgakopoulos, Panagiota Mitropoulou, Evangelia Koutli, Konstantinos Thomas, Marietta Charakida and Georgios Georgiopoulos*
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Investigating the link Between Psoriasis and Cardiovascular Disease: Current Evidence, Therapeutic Implications and Perspectives

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Eirini Kapniari*, Prokopios Papadimitriou, Marianna Dalamaga, George Makavos, Stefano Piaserico, Alexander Egeberg, Ignatios Ikonomidis and Evangelia Papadavid
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Uric Acid in Metabolic and Cerebrovascular Disorders: A Review

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Francesca Cortese*, Pietro Scicchitano, Anna M. Cortese, Giovanni Meliota, Andrea Andriani, Luigi Truncellito, Giacinto Calculli, Paola Giordano and Marco M. Ciccone
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The Endothelial Glycocalyx as a Key Mediator of Albumin Handling and the Development of Diabetic Nephropathy

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Emmanouil Korakas, Ignatios Ikonomidis, Konstantinos Markakis, Athanasios Raptis, George Dimitriadis and Vaia Lambadiari*
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Antipsychotic Drugs and Risk of Developing Venous Thromboembolism and Pulmonary Embolism: A Systematic Review and Meta-Analysis

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Omid Arasteh, Homa Nomani, Hamed Baharara, Seyed A. Sadjadi, Amir H. Mohammadpour*, Vahid Ghavami*, Thozhukat Sathyapalan and Amirhossein Sahebkar*
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Beta-Blockers and Cardiovascular Outcomes in Acute Heart Failure with a History of Coronary Artery Disease and an Ejection Fraction ≥ 40%

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Charbel Abi Khalil*, Kadhim Sulaiman, Nidal Asaad, Khalid F. AlHabib, Alawi Alsheikh-Ali, Mohammed Jameesh, Mohammed Al-Jarallah, Bassam Bulbanat, Wael AlMahmeed, Mustafa Ridha, Nooshin Bazargani, Haitham Amin, Ahmed Al-Motarreb, Husam AlFaleh, Prashanth Panduranga, Ziyad Mahfoud and Jassim Al Suwaidi
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LncRNA MALAT1 Enhances ox-LDL-Induced Autophagy Through the SIRT1/MAPK/NF-κB Pathway in Macrophages

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Jiaqi Yang, Xuze Lin , Li Liangshan Wang, Tienan Sun, Qi Zhao, Qian Ma* and Yujie Zhou*
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Screening for and Optimal Management of Small Abdominal Aortic Aneurysms: The Quest Continues promotion: free to download

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Kosmas I. Paraskevas*, Hans-Henning Eckstein, Andrew N. Nicolaides and George Geroulakos
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Acknowledgements to Reviewers promotion: free to download

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