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Sayeed-Desta, Naheed, Ajay Babu Pazhayattil, Jordan Collins, Shu Chen, Marzena Ingram und Jana Spes. „Assessment Methodology for Process Validation Lifecycle Stage 3A“. AAPS PharmSciTech 18, Nr. 5 (06.10.2016): 1881–86. http://dx.doi.org/10.1208/s12249-016-0641-9.
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Çiçek, Ekrem, Corneliu Cojocaru, Grazyna Zakrzewska-Trznadel, Marian Harasimowicz und Agnieszka Miskiewicz. „Response surface methodology for the modelling of85Sr adsorption on zeolite 3A and pumice“. Environmental Technology 33, Nr. 1 (Januar 2012): 51–59. http://dx.doi.org/10.1080/09593330.2010.549514.
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Fadda, Ahmed, Ezz Eldeen Kandeel und Eman El-Gendy. „Synthesis and antimicrobial evaluation of some new hydrazo, dihydropyridazinyl and triazolyl derivatives containing indole nucleus“. Pigment & Resin Technology 46, Nr. 2 (06.03.2017): 122–30. http://dx.doi.org/10.1108/prt-11-2015-0118.
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Purpose The aim of this paper is synthesis of some new hydrazo, dihydropyridazinyl and triazolyl derivatives containing indole nucleus and their antimicrobial evaluation. Design/methodology/approach Treatment of 3-(1H-indol-3-yl)-3-oxopropanenitrile (1) with different aryl diazonium salts 2a-j gave the corresponding arylazohydrazone derivatives 3a-j. The azo derivatives 3d and 3e were used as the key intermediate for the synthesis of some new diazines 5d, e and triazoles 7d, e. The newly synthesized compounds were characterized by electronic absorption properties – IR, 1HNMR and MS studies – and screened for their biological evaluation. Compounds 3a-j, 5d, e and 7d, e showed promising results as antimicrobial agents. Findings Compounds 3a-j, 5d, e and 7d, e showed promising results as antimicrobial agents. Originality/value No details regarding the synthesis of such dyes are reported before in the literature.
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Kamal, Mustafa, Arsalan Jamil Raja, Tanveer Ahmed, Mashhood Ali und Faisal Rasheed. „Efficacy of Sofosbuvir Plus Ribavirin with and without Pegylated Interferon-Α in Patients with HCV Genotype 3A Infection“. Pakistan Journal of Medical and Health Sciences 15, Nr. 7 (30.07.2021): 2272–74. http://dx.doi.org/10.53350/pjmhs211572272.
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Background: Hepatitis C virus (HCV) infection is a serious problem in low and middle income countries including Pakistan. Objective: To compare the efficacy of combination therapy, Sofosbuvir plus Ribavirin with and without Pegylated Interferon-α in HCV genotype 3a infected patients. Study Design: Randomized control trial Place and Duration: Department of Gastroenterology, Pakistan Institute of Medical Sciences (PIMS), Islamabad, during from 16th April 2017 to 15th October 2017. Methodology: One hundred and fifty four HCV infected patients with genotype 3a were included in this study. Detailed demographics were recorded after taking informed written consent. Patients were divided in two groups (A and B) randomly, Group A was offered with Sofosbuvir plus Ribavirin with Pegylated Interferon-α for 12 weeks and Group B was offered with Sofosbuvir plus Ribavirin for 24 weeks. The sustained virological response (SVR) after 12 weeks of therapy was compared between the study groups. Results: The frequency of SVR12 was comparatively higher in patients treated with Sofosbuvir plus Ribavirin with Pegylated Interferon-α (94.8%) than Sofosbuvir plus Ribavirin alone (84.4%) with similar trends in gender and age groups. Conclusion: The combination therapy Sofosbuvir plus Ribavirin with Pegylated Interferon-α had higher eradication rate against HCV genotype 3a in our local setting. Key Words: HCV, genotype 3a, Sofosbuvir, Ribavirin, Pegylated Interferon-α, SVR12
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Zhong, Yu-Jie, Jian-Hong Liao, Tzu-Hao Chiu, Yuh-Sheng Wen und C. W. Liu. „A New Synthetic Methodology in the Preparation of Bimetallic Chalcogenide Clusters via Cluster-to-Cluster Transformations“. Molecules 26, Nr. 17 (05.09.2021): 5391. http://dx.doi.org/10.3390/molecules26175391.
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A decanuclear silver chalcogenide cluster, [Ag10(Se){Se2P(OiPr)2}8] (2) was isolated from a hydride-encapsulated silver diisopropyl diselenophosphates, [Ag7(H){Se2P(OiPr)2}6], under thermal condition. The time-dependent NMR spectroscopy showed that 2 was generated at the first three hours and the hydrido silver cluster was completely consumed after thirty-six hours. This method illustrated as cluster-to-cluster transformations can be applied to prepare selenide-centered decanuclear bimetallic clusters, [CuxAg10-x(Se){Se2P(OiPr)2}8] (x = 0–7, 3), via heating [CuxAg7−x(H){Se2P(OiPr)2}6] (x = 1–6) at 60 °C. Compositions of 3 were accurately confirmed by the ESI mass spectrometry. While the crystal 2 revealed two un-identical [Ag10(Se){Se2P(OiPr)2}8] structures in the asymmetric unit, a co-crystal of [Cu3Ag7(Se){Se2P(OiPr)2}8]0.6[Cu4Ag6(Se){Se2P(OiPr)2}8]0.4 ([3a]0.6[3b]0.4) was eventually characterized by single-crystal X-ray diffraction. Even though compositions of 2, [3a]0.6[3b]0.4 and the previous published [Ag10(Se){Se2P(OEt)2}8] (1) are quite similar (10 metals, 1 Se2−, 8 ligands), their metal core arrangements are completely different. These results show that different synthetic methods by using different starting reagents can affect the structure of the resulting products, leading to polymorphism.
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Aljohani, Ghadah, Musa Said, Dieter Lentz, Norazah Basar, Arwa Albar, Shaya Alraqa und Adeeb Ali. „Microwave-Assisted Synthesis of Mono- and Disubstituted 4-Hydroxyacetophenone Derivatives via Mannich Reaction: Synthesis, XRD and HS-Analysis“. Molecules 24, Nr. 3 (07.02.2019): 590. http://dx.doi.org/10.3390/molecules24030590.
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An efficient microwave-assisted one-step synthetic route toward Mannich bases is developed from 4-hydroxyacetophenone and different secondary amines in quantitative yields, via a regioselective substitution reaction. The reaction takes a short time and is non-catalyzed and reproducible on a gram scale. The environmentally benign methodology provides a novel alternative, to the conventional methodologies, for the synthesis of mono- and disubstituted Mannich bases of 4-hydroxyacetophenone. All compounds were well-characterized by FT-IR, 1H NMR, 13C NMR, and mass spectrometry. The structures of 1-{4-hydroxy-3-[(morpholin-4-yl)methyl]phenyl}ethan-1-one (2a) and 1-{4-hydroxy-3-[(pyrrolidin-1-yl)methyl]phenyl}ethan-1-one (3a) were determined by single crystal X-ray crystallography. Compound 2a and 3a crystallize in monoclinic, P21/n, and orthorhombic, Pbca, respectively. The most characteristic features of the molecular structure of 2a is that the morpholine fragment adopts a chair conformation with strong intramolecular hydrogen bonding. Compound 3a exhibits intermolecular hydrogen bonding, too. Furthermore, the computed Hirshfeld surface analysis confirms H-bonds and π–π stack interactions obtained by XRD packing analyses.
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Mishra, Bhavesh Kumar, Uday Narayan Yadav, Saroj Khatiwada, Man Kumar Tamang, Shivir Dahal und Yi-Ping Li. „Hepatitis C virus genotype and its correlation with viral load in patients from Kathmandu, Nepal“. Journal of Infection in Developing Countries 14, Nr. 12 (31.12.2020): 1470–74. http://dx.doi.org/10.3855/jidc.10391.
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Introduction: Knowledge about the distribution of hepatitis C virus (HCV) genotype and its correlation with viral load are important for the decision of treatment and the prediction of disease progression, however such information is very limited in Nepal. Here, we investigated the distribution of HCV genotypes and viral load for HCV-infected patients from Kathmandu, Nepal.
Methodology: Ninety-six patients with HCV infection and not on antiviral therapy were enrolled from three different medical centers in Kathmandu valley, Nepal. Demographics were recorded and blood samples were collected. Plasma was separated and HCV RNA was extracted. Reverse transcriptase PCR (RT-PCR) was performed to measure the viral load, and virus genotype was determined.
Results: Genotype 3a (n = 53, 55.2%) was the most prevalent, followed by 1b (n = 19, 19.8%), 1a (n = 18, 18.8%), 5a (n = 3, 3.1%), and mix types (n = 3, 3.1%). The median viral load for HCV genotype 1a was 770,942 IU/mL (IQR, 215,268-3,720,075), 1b was 700,000 IU/mL (IQR, 431,560-919,000), 3a was 1,060,000 IU/mL (IQR, 641,050-6,063,500), 5a was 673,400 IU/mL, and mixed was 6,428,000 IU/mL. A correlation between genotype and viral load was observed (p = 0.02), of which genotype 3a showed a high viral load.
Conclusions: HCV genotypes 1a, 1b, 3a, and 5a were identified in Kathmandu, Nepal, and mixed genotype patients were observed in the patients studied. HCV genotype showed a correlation with viral load in patient plasma. This finding may contribute to the treatment and prevention of hepatitis C in Kathmandu, Nepal.
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Joshi, Dhruval J., Meesook Jun, Lijing Yang, Alan J. Lough und Hongbin Yan. „Further investigation on the nitration of BODIPY with cupric nitrate: crystal structures of 4,4-difluoro-1,3,5,7,8-pentamethyl-2-nitro-4-bora-3a,4a-diaza-s-indacene, 4,4-difluoro-3-nitro-8-phenyl-4-bora-3a,4a-diaza-s-indacene, and 3-chloro-6-ethyl-5,7,8-trimethyl-2-nitro-4,4-diphenyl-4-bora-3a,4a-diaza-s-indacene“. Acta Crystallographica Section E Crystallographic Communications 74, Nr. 2 (09.01.2018): 103–8. http://dx.doi.org/10.1107/s2056989017018564.
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The treatment of non-fully substituted 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene (BODIPY) with cupric nitrate leads to the introduction of a nitro group at different positions of the BODIPY core, depending on the substitution pattern. This methodology complements the treatment of fully substituted BODIPY with cupric nitrate that was previously reported. The crystal structures of 4,4-difluoro-1,3,5,7,8-pentamethyl-2-nitro-4-bora-3a,4a-diaza-s-indacene, C14H16BF2N3O2 (5a) 4,4-difluoro-3-nitro-8-phenyl-4-bora-3a,4a-diaza-s-indacene, C15H10BF2N3O2 (5b) and 3-chloro-6-ethyl-5,7,8-trimethyl-2-nitro-4,4-diphenyl-4-bora-3a,4a-diaza-s-indacene, C26H25BClN3O2 (5d) are presented. In all three structures, the fused ring system is in a very flattened `V-shape', with dihedral angles between the two outer five membered rings of 8.12 (14), 6.67 (9) and 12.30 (18) Å for 5a, 5b and 5d, respectively. In each case, the central six-membered ring is in a flattened sofa conformation. In the crystal of 5a, molecules are linked by weak C—H...O and C—H...F hydrogen bonds forming sheets parallel to (10-1). In the crystal of 5b molecules are linked by weak C—H...O and C—H...F hydrogen bonds and π–π interactions forming sheets parallel to (001). In the crystal of 5d, weak C—H...O hydrogen bonds link molecules into chains along [001]. In compound 5d, the atoms of the nitro group were refined as disordered over two sets of sites with occupancies 0.618 (12) and 0.382 (12).
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Wallander, Michelle L., Katherine B. Geiersbach, Sheryl R. Tripp und Lester J. Layfield. „Comparison of Reverse Transcription-Polymerase Chain Reaction, Immunohistochemistry, and Fluorescence In Situ Hybridization Methodologies for Detection of Echinoderm Microtubule-Associated Proteinlike 4–Anaplastic Lymphoma Kinase Fusion–Positive Non–Small Cell Lung Carcinoma: Implications for Optimal Clinical Testing“. Archives of Pathology & Laboratory Medicine 136, Nr. 7 (01.07.2012): 796–803. http://dx.doi.org/10.5858/arpa.2011-0321-oa.
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Context.—Echinoderm microtubule–associated proteinlike 4–anaplastic lymphoma kinase (EML4-ALK) gene fusions are detected in 3% to 13% of non–small cell lung carcinomas. Accurate testing for detection of EML4-ALK fusions is essential for appropriate therapy selection. Objective.—To compare reverse transcription-polymerase chain reaction (RT-PCR), immunohistochemistry (IHC), and fluorescence in situ hybridization (FISH) methodologies for detection of EML4-ALK fusions. Design.—Forty-six pulmonary adenocarcinomas were selected with enrichment for wild-type epidermal growth factor receptor (EGFR) status (wild type, n = 42; mutant, n = 4). Specimens were tested by IHC (Dako; clone ALK1), FISH (Abbott Molecular; LSI ALK break apart), and RT-PCR (variants 1 and 3a/b). Results.—EML4-ALK variant 3a/b was detectable by RT-PCR, FISH, and IHC in 4% (2 of 46) of specimens. Complete agreement among FISH and IHC reviewers was obtained for variant 3a/b. No concordance existed among methodologies for the detection of EML4-ALK variant 1. The RT-PCR method detected variant 1 in 20% (9 of 46) of specimens. Agreement among FISH viewers was poor for variant 1 because only 11% (1/9) of specimens were scored as positive by all 3 viewers. The sensitivity of IHC for detection of variant 1 was also poor because only 1 of 9 samples (11%) was scored as positive. Overall, the frequency of EML4-ALK variants 1 and 3a/b was 24% (11 of 46) in adenocarcinomas enriched for wild-type EGFR status. One EML4-ALK variant 1 fusion was found to coexist with an EGFR exon 21 mutation. Conclusions.—The FISH interpretation demonstrated great variability among observers. The RT-PCR method was the most sensitive and least-subjective methodology for detection of EML4-ALK fusions.
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Zhang, Xuejiao, Yihong Hu, Chenzhong Jin und Weiguo Wu. „Extraction and Hypolipidemic Activity of Low Molecular Weight Polysaccharides Isolated from Rosa Laevigata Fruits“. BioMed Research International 2020 (22.10.2020): 1–20. http://dx.doi.org/10.1155/2020/2043785.
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Three novel low molecular weight polysaccharides (RLP-1a, RLP-2a, and RLP-3a) with 9004, 8761, and 7571 Da were first obtained by purifying the crude polysaccharides from the fruits of a traditional Chinese medicinal herb Rosae Laevigatae. The conditions for polysaccharides from the R. Laevigatae fruit (RLP) extraction were optimized by the response surface methodology, and the optimal conditions were as follows: extraction temperature, 93°C; extraction time, 2.8 h; water to raw material ratio, 22; extraction frequency, 3. Structural characterization showed that RLP-1a consisted of rhamnose, arabinose, xylose, glucose, and galactose with the ratio of 3.14 : 8.21 : 1 : 1.37 : 4.90, whereas RLP-2a was composed of rhamnose, mannose, glucose, and galactose with the ratio of 1.70 : 1 : 93.59 : 2.73, and RLP-3a was composed of rhamnose, arabinose, xylose, mannose, glucose, and galactose with the ratio of 6.04 : 26.51 : 2.05 : 1 : 3.17 : 31.77. The NMR analyses revealed that RLP-1a, RLP-2a, and RLP-3a contained 6, 4, and 6 types of glycosidic linkages, respectively. RLP-1a and RLP-3a exhibited distinct antioxidant abilities on the superoxide anions, 1,1-diphenyl-2-picrylhydrazyl (DPPH), and hydroxyl radicals in vitro. RLPs could decrease the serum lipid levels, elevate the serum high-density lipoprotein cholesterol levels, enhance the antioxidant enzymes levels, and upregulate of FADS2, ACOX3, and SCD-1 which involved in the lipid metabolic processes and oxidative stress in the high-fat diet-induced rats. These results suggested that RLPs ameliorated the high-fat diet- (HFD-) induced lipid metabolism disturbance in the rat liver through the peroxisome proliferator-activated receptor (PPAR) signaling pathway. Low molecular weight polysaccharides of RLP could be served as a novel potential functional food for improving hyperlipidemia and liver oxidative stress responses.
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Roopan, Selvaraj Mohana, Annadurai Bharathi und Duraipandi Devi Priya. „Microwave Assisted Synthesis and Its Cytotoxicity Study of 4H-Pyrano[2,3-a]acridine-3-carbonitrile Intermediate: Experiment Design for Optimization Using Response Surface Methodology“. Proceedings 41, Nr. 1 (14.11.2019): 12. http://dx.doi.org/10.3390/ecsoc-23-06594.
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Several synthetic routes have been achieved to synthesize pyrane fused systems. As a follow up of earlier work, we hereby report the microwave assisted synthesis of key intermediate, pyrane fused acridine compounds 3a–f. It was obtained by treating α,β-unsaturated ketone 1a–f and malononitrile 2 in presence of piperidine with ethanolic solution at 50 C under 200 W power. This method also optimized via microwave method using RSM methodology. All the synthesized derivatives and target compounds were evaluated for cytotoxicity effect on human hepatoblastoma (HepG2) cell line and HDAC enzyme activity.
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Yan, Fei, Yonglei Cui, Yue An, Jing Ning, Xinyu Zhao, Lei Feng, Xiaokui Huo et al. „A dual functional probe for assessing human CYP450 3A5 and 3A enzymes bioactivities“. Future Medicinal Chemistry 11, Nr. 22 (November 2019): 2891–903. http://dx.doi.org/10.4155/fmc-2019-0173.
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Aim: CYP3A5 plays a vital role in the drug metabolism, it displays varied expression levels among individuals and is easily influenced by genetic polymorphisms and some diseases. Methodology & results: A dual function probe isobutyryl-11-keto- β-boswellic acid (IKBA) was developed; it possessed a high selectivity toward CYP3A5 and CYP3A enzymes for its two individual metabolites, respectively. The probe has the high accuracy and wide applicability in measuring the real activity of CYP3A5. Finally, IKBA was successfully used for the evaluation of the activity of CYP3A5 and CYP3A enzymes in various bio samples. Conclusion: IKBA could serve as a useful tool for exploring the physiology and pathology functions of CYP3A5 and give some useful guidance for the rational use of clinical drugs.
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Clerc, Sébastien, Craig Donlon, Franck Borde, Nicolas Lamquin, Samuel E. Hunt, Dave Smith, Malcolm McMillan et al. „Benefits and Lessons Learned from the Sentinel-3 Tandem Phase“. Remote Sensing 12, Nr. 17 (19.08.2020): 2668. http://dx.doi.org/10.3390/rs12172668.
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During its commissioning phase, the Copernicus Sentinel-3B satellite has been placed in a tandem formation with Sentinel-3A for a period of 6 months. This configuration allowed a direct comparison of measurements obtained by the two satellites. The purpose of this paper was to present the range of analyses that can be performed from this dataset, highlighting methodology aspects and the main outcomes for each instrument. We examined, in turn, the benefit of the tandem in understanding instrument operational modes differences, in assessing inter-satellite differences, and in validating measurement uncertainties. The results highlighted the very good consistency of the Sentinel-3A and B instruments, ensuring the complete inter-operability of the constellation. Tandem comparisons also pave the way for further improvements through harmonization of the sensors (OLCI), correction of internal stray-light sources (SLSTR), or high-frequency processing of SRAL SARM data. This paper provided a comprehensive overview of the main results obtained, as well as insights into some of the results. Finally, we drew the main lessons learned from the Sentinel-3 tandem phase and provided recommendations for future missions.
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Tasqeeruddin, S., Yahya I. Asiri und S. Shaheen. „Zirconium(IV) Oxychloride: A Simple and Efficient Catalyst for the Synthesis of Chromen-2-one Derivatives“. Asian Journal of Chemistry 32, Nr. 10 (2020): 2611–16. http://dx.doi.org/10.14233/ajchem.2020.22849.
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The present work explores a highly efficient, environmental friendly, green protocol for the synthesis of chromen-2-one derivatives (3a-m) by the condensation of salicylaldehydes with various active methylene compounds using zirconium (IV) oxychloride as catalyst. This is a convenient and rapid method for Knoevenagel condensation and this methodology offers several advantages including shorter reaction time, milder conditions, inexpensive catalyst, simple operational procedure and allowed to achieve the desired products in excellent yields. The structures of all the synthesized compounds were confirmed by spectral data.
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Lu, Qifeng, William Bell, Peter Bauer, Niels Bormann und Carole Peubey. „Characterizing the FY-3A Microwave Temperature Sounder Using the ECMWF Model“. Journal of Atmospheric and Oceanic Technology 28, Nr. 11 (01.11.2011): 1373–89. http://dx.doi.org/10.1175/jtech-d-10-05008.1.
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Abstract China’s Feng-Yun-3A (FY-3A), launched in May 2008, is the first in a series of seven polar-orbiting meteorological satellites planned for the next decade by China. The FY-3 series is set to become an important data source for numerical weather prediction (NWP), reanalysis, and climate science. FY-3A is equipped with a microwave temperature sounding instrument (MWTS). This study reports an assessment of the MWTS instrument using the ECMWF NWP model, radiative transfer modeling, and comparisons with equivalent observations from the Advanced Microwave Sounding Unit-A (AMSU-A). The study suggests the MWTS instrument is affected by biases related to large shifts, or errors, in the frequency of the channel passbands as well as radiometer nonlinearity. The passband shifts, relative to prelaunch measurements, are 55, 39, and 33 MHz for channels 2–4, respectively. Relative to the design specification the shifts are 60, 80, and 83 MHz, with uncertainties of ±2.5 MHz. The radiometer nonlinearity results in a positive bias in measured brightness temperatures and is manifested as a quadratic function of measured scene temperatures. By correcting for both of these effects the quality of the MWTS data is improved significantly, with the standard deviations of the (observed minus simulated) differences based on short-range forecast fields reduced by 30%–50% relative to simulations using prelaunch measurements of the passband, to values close to those observed for AMSU-A-equivalent channels. The new methodology could be applied to other microwave temperature sounding instruments and illustrates the value of NWP fields for the on-orbit characterization of satellite sensors.
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Correa, Christian, María del Carmen Cruz, Fabiola Jiménez, L. Gerardo Zepeda und Joaquín Tamariz. „A New Synthetic Route of 2-Aroyl- and 2-Benzyl-Benzofurans and their Application in the Total Synthesis of a Metabolite Isolated from Dorstenia gigas“. Australian Journal of Chemistry 61, Nr. 12 (2008): 991. http://dx.doi.org/10.1071/ch08243.
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The Lewis acid-catalyzed cyclization of the (Z)-3-(dimethylamino)-2-aryloxy-1-arylprop-2-en-1-ones 4a–h leads to a regioselective and short synthesis of 2-aroylbenzofurans 2a–h. The Wolff–Kishner reduction of the latter yielded a series of substituted 2-benzylbenzofurans 3a–h. This methodology was applied in the first total synthesis of the metabolite 2-(4-hydroxybenzyl)-6-methoxybenzofuran 1, which was isolated from the tropical plant Dorstenia gigas, and obtained through a six-step route and in a 24% overall yield.
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Smith, Dave, Marc Barillot, Stephane Bianchi, Fabio Brandani, Peter Coppo, Mireya Etxaluze, Johannes Frerick et al. „Sentinel-3A/B SLSTR Pre-Launch Calibration of the Thermal InfraRed Channels“. Remote Sensing 12, Nr. 16 (05.08.2020): 2510. http://dx.doi.org/10.3390/rs12162510.
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The first two models of the Sea and Land Surface Temperature Radiometers (SLSTR) for the European Copernicus Sentinel-3 missions were tested prior to launch at the Rutherford Appleton Laboratory space instrument calibration facility. The pre-launch tests provide an essential reference that ensures that the flight data of SLSTR are calibrated to the same standards needed for surface temperature measurements and to those used by shipborne radiometers for Fiducial Reference Measurement (FRM). The radiometric calibrations of the thermal infrared channels were validated against accurate and traceable reference BB sources under flight representative thermal vacuum environment. Measurements were performed in both earth views for source temperatures covering the main operating range, for different instrument configurations and for the full field-of-view of the instruments. The data were used to derive non-linearity curves to be used in the level-1 processing. All results showed that the measured brightness temperatures and radiometric noise agreed within the requirements for the mission. An inconsistency that particularly affected SLSTR-A was observed which has been attributed to an internal stray light error. A correction for the stray light has been proposed to reduce the error. The internal stray light error was reduced for SLSTR-B by replacing the coating on the main aperture stop. We present a description of the test methodology and the key results.
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Taheri Afarani, Hajar, Morteza Sadeghi, Ahmad Moheb und Ebrahim Nasr Esfahani. „Optimization of the gas separation performance of polyurethane–zeolite 3A and ZSM-5 mixed matrix membranes using response surface methodology“. Chinese Journal of Chemical Engineering 27, Nr. 1 (Januar 2019): 110–29. http://dx.doi.org/10.1016/j.cjche.2018.03.013.
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Goshvarpour, Ateke, Atefeh Goshvarpour und Ataollah Abbasi. „Integration of Wavelet and Recurrence Quantification Analysis in Emotion Recognition of Bilinguals“. International Clinical Neuroscience Journal 7, Nr. 1 (13.12.2019): 35–45. http://dx.doi.org/10.15171/icnj.2020.06.
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Background: This study offers a robust framework for the classification of autonomic signals into five affective states during the picture viewing. To this end, the following emotion categories studied: five classes of the arousal-valence plane (5C), three classes of arousal (3A), and three categories of valence (3V). For the first time, the linguality information also incorporated into the recognition procedure. Precisely, the main objective of this paper was to present a fundamental approach for evaluating and classifying the emotions of monolingual and bilingual college students. Methods: Utilizing the nonlinear dynamics, the recurrence quantification measures of the wavelet coefficients extracted. To optimize the feature space, different feature selection approaches, including generalized discriminant analysis (GDA), principal component analysis (PCA), kernel PCA, and linear discriminant analysis (LDA), were examined. Finally, considering linguality information, the classification was performed using a probabilistic neural network (PNN). Results: Using LDA and the PNN, the highest recognition rates of 95.51%, 95.7%, and 95.98% were attained for the 5C, 3A, and 3V, respectively. Considering the linguality information, a further improvement of the classification rates accomplished. Conclusion: The proposed methodology can provide a valuable tool for discriminating affective states in practical applications within the area of human-computer interfaces.
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Shehzad, Muhammad Tariq, Ajmal Khan, Sobia Ahsan Halim, Abdul Hameed, Aqeel Imran, Jamshed Iqbal, Aziz Ullah et al. „Synthesis of indole-substituted thiosemicarbazones as an aldose reductase inhibitor: an in vitro, selectivity and in silico study“. Future Medicinal Chemistry 13, Nr. 14 (Juli 2021): 1185–201. http://dx.doi.org/10.4155/fmc-2020-0060.
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Aim: Indole is an important component of many drug molecules, and its conjugation with thiosemicarbazone moiety would be advantageous in finding lead compounds for the development of diabetic complications. Methodology: We have designed, synthesized and evaluated a series of 17 indole-thiosemicarbazones (3a–q) as aldose reductase (ALR2) and aldehyde reductase (ALR1) inhibitors. Results: After in vitro evaluation, all indole-thiosemicarbazones showed significant inhibition against both enzyme ALR1 and ALR2 with IC50 in range of 0.42–20.7 and 1.02–19.1 μM, respectively. The docking study was also carried out to consider the putative binding of molecules with the target enzymes. Conclusion: Compound 3f was found to be most active and selective for ALR2. The indole-thiosemicarbazones series described here has selective hits for diabetes-mellitus-associated complications.
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Schlachter, Adrien, Alexandre Fleury, Kevin Tanner, Armand Soldera, Benoit Habermeyer, Roger Guilard und Pierre D. Harvey. „The TDDFT Excitation Energies of the BODIPYs; The DFT and TDDFT Challenge Continues“. Molecules 26, Nr. 6 (22.03.2021): 1780. http://dx.doi.org/10.3390/molecules26061780.
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The derivatives of 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene (BODIPY) are pivotal ingredients for a large number of functional, stimuli-responsive materials and therapeutic molecules based on their photophysical properties, and there is a urgent need to understand and predict their optical traits prior to investing a large amount of resources in preparing them. Density functional theory (DFT) and time-dependent DFT (TDDFT) computations were performed to calculate the excitation energies of the lowest-energy singlet excited state of a large series of common BODIPY derivatives employing various functional aiming at the best possible combination providing the least deviations from the experimental values. Using the common “fudge” correction, a series of combinations was investigated, and a methodology is proposed offering equal or better performances than what is reported in the literature.
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Revanasiddappa, B. C., M. Vijay Kumar und Hemanth Kumar. „Synthesis and Antioxidant activity of novel Pyrazoline derivatives“. Hygeia J. D.Med.10 (1) August 2018 - January 2019 10, Nr. 1 (15.09.2018): 43–49. http://dx.doi.org/10.15254/h.j.d.med.10.2018.177.
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Plan: A novel series of pyrazolines were synthesized through chalcones. The synthesized compounds were evaluated for various antioxidant activities. Preface: Pyrazolines belongs to five-membered nitrogen classes of compounds. Pyrazolines were reported with widespread chemotherapeutic activities. Methodology: A new series of Chalcones (2a-j) were prepared by reacting substituted aldehydes and ketones in alcohol medium in presence of NaOH. The chalcones (2a-j) undergoes selective cyclization with benzhydrazide (1) in glacial acetic acid medium to yield the title compounds 1, 3, 5-trisubstituted Pyrazolines (3a-j). The new compounds were assigned on the basis of 1H-NMR, IR and Mass spectral data. The newly synthesized compounds were screened for their In-Vitro antioxidant activity by DPPH, superoxide and nitric oxide methods. Outcome: Some of the tested compounds 3e, 3g, and 3f showed moderate activity when compared to the standard drug ascorbic acid.
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Demir, Ayhan S., Zuhal Gercek, Nese Duygu, A. Cigdem Igdir und Omer Reis. „Butenolide annelation using a manganese(III) oxidation. A synthesis of chromolaenin (Laevigatin)“. Canadian Journal of Chemistry 77, Nr. 8 (01.08.1999): 1336–39. http://dx.doi.org/10.1139/v99-136.
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A procedure was developed for the annelation of a butenolide to an aromatic ketone that highlighted a manganese(III) oxidation of an aromatic ketone. The merit of this procedure was illustrated in a synthesis of Chromolaenin (Laevigatin) (1) from 4,7-dimethyl-1-tetralone (2c). Oxidation of tetralone and indanone with manganese(III) acetate in the presence of chloro- or bromopropionic acid or their Mn(II) salts furnished a α-haloesters 3a-d. An Arbuzov reaction of haloesters with triethylphosphite and an intramolecular Horner-Watsworth-Emmons cyclization of the resulting phosphonate gave butenolide 5a, b in 77-79% yield. This methodology was also applied to 4,7-dimethyl-1-tetralone (2c), and the corresponding butenolide 6 is synthesized in 85% yield, which was then converted to Chromolaenin (1) using DIBAL-H.Key words: chromolaenin (Laevigatin), manganese(III) acetate oxidation, aromatic ketones, butenolide annelation, lactone, Horner-Watsworth-Emmons cyclization, Arbuzov reaction.
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Lamquin, Nicolas, Sébastien Clerc, Ludovic Bourg und Craig Donlon. „OLCI A/B Tandem Phase Analysis, Part 1: Level 1 Homogenisation and Harmonisation“. Remote Sensing 12, Nr. 11 (03.06.2020): 1804. http://dx.doi.org/10.3390/rs12111804.
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Copernicus is a European system for monitoring the Earth in support of European policy. It includes the Sentinel-3 satellite mission which provides reliable and up-to-date measurements of the ocean, atmosphere, cryosphere, and land. To fulfil mission requirements, two Sentinel-3 satellites are required on-orbit at the same time to meet revisit and coverage requirements in support of Copernicus Services. The inter-unit consistency is critical for the mission as more S3 platforms are planned in the future. A few weeks after its launch in April 2018, the Sentinel-3B satellite was manoeuvred into a tandem configuration with its operational twin Sentinel-3A already in orbit. Both satellites were flown only thirty seconds apart on the same orbit ground track to optimise cross-comparisons. This tandem phase lasted from early June to mid October 2018 and was followed by a short drift phase during which the Sentinel-3B satellite was progressively moved to a specific orbit phasing of 140° separation from the sentinel-3A satellite. In this paper, an output of the European Space Agency (ESA) Sentinel-3 Tandem for Climate study (S3TC), we provide a full methodology for the homogenisation and harmonisation of the two Ocean and Land Colour Instruments (OLCI) based on the tandem phase. Homogenisation adjusts for unavoidable slight spatial and spectral differences between the two sensors and provide a basis for the comparison of the radiometry. Persistent radiometric biases of 1–2% across the OLCI spectrum are found with very high confidence. Harmonisation then consists of adjusting one instrument on the other based on these findings. Validation of the approach shows that such harmonisation then procures an excellent radiometric alignment. Performed on L1 calibrated radiances, the benefits of harmonisation are fully appreciated on Level 2 products as reported in a companion paper. Whereas our methodology aligns one sensor to behave radiometrically as the other, discussions consider the choice of the reference to be used within the operational framework. Further exploitation of the measurements indeed provides evidence of the need to perform flat-fielding on both payloads, prior to any harmonisation. Such flat-fielding notably removes inter-camera differences in the harmonisation coefficients. We conclude on the extreme usefulness of performing a tandem phase for the OLCI mission continuity as well as for any optical mission to which the methodology presented in this paper applies (e.g., Sentinel-2). To maintain the climate record, it is highly recommended that the future Sentinel-3C and Sentinel-3D satellites perform tandem flights when injected into the Sentinel-3 time series.
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Abdo, Nadia Y. Megally, Rafat M. Mohareb und Waleed N. Al-darkazali. „Heterocyclization of 2-Arylidenecyclohexan-1,3-dione: Synthesis of Thiophene, Thiazole, and Isoxazole Derivatives with Potential Antitumor Activities“. Anti-Cancer Agents in Medicinal Chemistry 20, Nr. 3 (24.04.2020): 335–45. http://dx.doi.org/10.2174/1871520619666190730103425.
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Background: Thiophene, thiazole, and isoxazole derivatives are present in a wide range of natural and synthetic compounds with heterogeneous pharmacological activity. Due to their structural diversity, they are some of the most versatile classes of compounds for anticancer drug design and discovery. Objective: Thiophene, thiazole, and isoxazole derivatives were herein designed with a dual purpose: as antiproliferative agents and kinase inhibitors. Methods: The test compounds were synthesized in moderate to high yields through a simple methodology. Tetrahydrobenzo[b]thiophen-5-one derivatives 5a-f were prepared from the reaction of 2-arylidencyclohexan- 1,3-dione 3a-c with elemental sulfur and either of malononitrile (4a) or ethyl cyanoacetate (4b) in 1,4-dioxan in the presence of triethylamine. Compounds 5a,b were used for the synthesis of thiophene, thiazole, and isoxazole derivatives through their reactions with different chemical reagents. Results: Antiproliferative evaluations, c-Met kinase, and Pim-1 kinase inhibitions were performed where some compounds revealed high activities. In all cases, antiproliferative activity and the kinase inhibitions were performed against six cancer cell lines and five tyrosine kinases, respectively. Where the most cytotoxic compounds were 3c, 5d, and 16c with IC50’s 0.29, 0.68, and 0.42μM, respectively, against the A549 cell line. Conclusion: The anti-proliferative activities of the newly synthesized compounds were evaluated against the six cancer cell lines (A549, HT-29, MKN-45, U87MG, SMMC-7721, and H460). The most potent compounds toward the cancer cell lines (3a, 3c, 5d, 7c, 11c, 16a, and 16c) were further investigated towards the five tyrosine kinases (c-kit, FIT-3, VEGFR-2, EGFR, and PDGFR). Compounds 3c, 5d, and 16c were selected for testing of their inhibition for the Pim-1 kinase due to their anti-proliferation activities against the cancer cell lines and their high activities against the tyrosine kinases.
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Giubellina, Nicola, Wim Aelterman und Norbert De Kimpe. „Use of 3-halo-1-azaallylic anions in heterocyclic chemistry“. Pure and Applied Chemistry 75, Nr. 10 (01.01.2003): 1433–42. http://dx.doi.org/10.1351/pac200375101433.
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The synthetic potential of lithio 3-halo-1-azaallylic anions as building blocks in organic chemistry and especially in heterocyclic chemistry will be highlighted by the synthesis of functionalized imines, obtained after reaction of 3-halo-1-azaallylic anions with het- eroatom-substituted electrophiles. Thus, the latter generated functionalized imines are suitable building blocks for the synthesis of a whole range of heterocycles and physiologically active compounds, including agrochemicals and pharmaceuticals. 3-Halo-1-azaallylic anions were used in the synthesis of N-alkyl-3,3-dichloroazetidines, 2,3-disubstituted pyrroles, piperidines, 2-substituted pyridines, 2-alkoxytetrahydrofurans,etc., from which a large range of useful and interesting chemicals can be produced, e.g., 2-azetines and 9-alkyl- 2-phenyl-3a-beta,4,6,7,8,9,9a-beta,9b-beta-octahydro-1H-pyrrolo [3,4,h]quinoline-1,3-diones. The utility of the present methodology is demonstrated by the synthesis of the pheromone (S)-manicone, the sulfur-containing flavor compound 2-[(methylthio)methyl ]-2-butenal, and some agrochemical and pharmaceutical compounds.
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Sharma, Neeraj, Neeraj Ahuja, Rachin Goyal und Vinod Rohilla. „Parametric optimization of EDD using RSM-Grey-TLBO-based MCDM approach for commercially pure titanium“. Grey Systems: Theory and Application 10, Nr. 2 (06.04.2020): 231–45. http://dx.doi.org/10.1108/gs-01-2020-0008.
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PurposeElectric discharge drilling (EDD) is used to drill quality microholes on any conductive materials. EDD process parameters play a crucial role in the drilling. Depending upon the material characteristics, the cost of drilling also changes. Therefore, a suitable method is required to control the process parameters and drill quality microholes.Design/methodology/approachThe input process parameters in the present work are peak current (Ip), pulse on-time (Ton) and pulse off-time (Toff). The trials were intended in accordance to central composite face-centered design of response surface methodology (RSM). The output responses, namely drilling rate (DR) and electrode wear ratio (EWR), were converted into a single response, that is, grade using Grey relational analysis (GRA). The grade value is further modeled by regression analysis. The empirical model was figured out using teaching–learning-based optimization (TLBO). The RSM-Grey-TLBO-based multicriteria decision-making (MCDM) is used to investigate the optimized process parameter setting.FindingsThe RSM-Grey-TLBO-based MCDM approach suggests that the optimized setting for DR and EWR is Ip: 3A; Ton: 40 µs; Toff: 42 µs. The percentage errors for the predicted and experimental results are 8.1 and 7.5% in DR and EWR, respectively.Originality/valueThe parametric optimization of EDD using RSM-Grey-TLBO-based MCDM approach while machining commercially pure titanium is still underway. Thus, this MCDM approach will give a path to the researchers working in this direction.
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Sobrino, José Antonio, und Itziar Irakulis. „A Methodology for Comparing the Surface Urban Heat Island in Selected Urban Agglomerations Around the World from Sentinel-3 SLSTR Data“. Remote Sensing 12, Nr. 12 (25.06.2020): 2052. http://dx.doi.org/10.3390/rs12122052.
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Retrieval of land surface temperature (LST) from satellite data allows to estimate the surface urban heat island (SUHI) as the difference between the LST obtained in the urban area and the LST of its surroundings. However, this definition depends on the selection of the urban and surroundings references, which translates into greater difficulty in comparing SUHI values in different urban agglomerations across the world. In order to avoid this problem, a methodology is proposed that allows reliable quantification of the SUHI. The urban reference is obtained from the European Space Agency Climate Change Initiative Land Cover and three surroundings references are considered; that is, the urban adjacent (Su), the future adjacent (Sf), and the peri-urban (Sp), which are obtained from mathematical expressions that depend exclusively on the urban area. In addition, two formulations of SUHI are considered: SUHIMAX and SUHIMEAN, which evaluate the maximum and average SUHI of the urban area for each of the three surrounding references. As the urban population growth phenomenon is a world-scale problem, this methodology has been applied to 71 urban agglomerations around the world using LST data obtained from the sea and land surface temperature radiometer (SLSTR) on board Sentinel-3A. The results show average values of SUHIMEAN of (1.8 ± 0.9) °C, (2.6 ± 1.3) °C, and (3.1 ± 1.7) °C for Su, Sf, and Sp, respectively, and an average difference between SUHIMAX and SUHIMEAN of (3.1 ± 1.1) °C. To complete the study, two additional indices have been considered: the Urban Thermal Field Variation Index (UFTVI) and the Discomfort Index (DI), which proved to be essential for understanding the SUHI phenomenon and its consequences on the quality of life of the inhabitants.
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Elaiyarasan, Uthirapathi, Vinaitheerthan Satheeshkumar und Chinnamuthu Senthilkumar. „An investigation on electrical discharge metal matrix coating of ZE41A magnesium alloy“. Metallurgical Research & Technology 118, Nr. 3 (2021): 314. http://dx.doi.org/10.1051/metal/2021034.
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The present paper studied the experimental investigation on electrical discharge coating of ZE41A magnesium alloy (EDC) with tungsten carbide-copper (WC/Cu) powder metallurgy (PM) electrode. In order to attain the surface characteristics, three parameters were selected such as compaction load, current and pulse on time. Response characteristics such as material transfer rate (MTR) and surface roughness (Ra) were considered in this study. Central composite design in response surface methodology was applied to conduct experiments. Empirical models were developed for MTR and SR. AVOVA test was conducted to identify the most influence parameters. Additionally, optimized parameters were identified by response surface optimizer. It is observed that the current play a vital role in increasing the MTR and minimize the SR of the coated surface followed by compaction load and pulse on time. Various studies such as scanning electron microscopy (SEM) and energy dispersive spectroscopy (EDS) were carried out on the coated surface. Bulk mass deposition and bigger craters were observed in the surface coated with 150 MPa and 3A respectively.
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Akhund, Anwar Ali, Rehana Akhtar, Syed Qaiser Husain Naqvi und Mustafa Kamal. „CHRONIC HEPATITIS;“. Professional Medical Journal 21, Nr. 03 (10.06.2014): 450–54. http://dx.doi.org/10.29309/tpmj/2014.21.03.2032.
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Objective: To determine the correlation between HCV genotypes and serum ALTlevels in various patients of chronic hepatitis induced by hepatitis C virus, in our setup. Design: Aprospective study carried out from August 2006 to December 2009. Setting: Research MedicalCenter LUMHS Jamshoro, Pathology Department Peoples University of Medical & HealthSciences Nawabshah and Biotechnology Department University of Karachi. Patients: A total of344 HCV-PCR positive patients with different genotypes were evaluated 239 men and 105 womenwith ages between 18–55 years of age years were included in the study. Methodology: All thepatients went for ELISA test for the presence of HCV antibodies by ELISA kit of Biokit Spain, then a10.0 ml sample of blood was collected in a tube with separating gel, to obtain serum, which wasO stored at -80 C, for the determination of HCV RNA by RT- PCR (Real time cephid smart cycler) andfor determination of HCV-RNA genotypes by comparison in sizes of the products amplified by RTPCRusing HCV genotype- specific primers, then subjecting the product to electrophoresis byAnagen kit. 5.0 ml of blood was also collected in a tube with separating gel, to obtain serum,which was stored at room temperature for the determination alanine aminotransferase by usingUV enzymatic kinetic method. Results: when HCV genotypes were correlated with serum ALTlevels, 09 cases were found < 50 mg % and among these 06 cases were of genotype 1a, 02 caseswere of genotype 2a and one case of untyped. 55 cases shows serum ALT level between 50-100mg % and among this majority of cases belongs to untyped category. 209 cases shows serumALT level between 100-200 mg % and among this majority of cases belongs to genotype 3a. 71cases shows serum ALT level >200 mg % and among this majority of cases belongs to genotype3a. Conclusions: The data in the current study indicates the strong correlation between HCVgenotypes and serum ALT levels. The genotypes 3a, 3b and 2 were found associated with highserum ALT levels and the genotype 1 was found associated with low levels of serum ALT.
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Krasuski, Kamil, Dariusz Popielarczyk, Adam Ciećko und Janusz Ćwiklak. „A New Strategy for Improving the Accuracy of Aircraft Positioning Using DGPS Technique in Aerial Navigation“. Energies 14, Nr. 15 (22.07.2021): 4431. http://dx.doi.org/10.3390/en14154431.
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In this paper a new mathematical algorithm is proposed to improve the accuracy of DGPS (Differential GPS) positioning using several GNSS (Global Navigation Satellites System) reference stations. The new mathematical algorithm is based on a weighting scheme for the following three criteria: weighting in function of baseline (vector) length, weighting in function of vector length error and weighting in function of the number of tracked GPS (Global Positioning System) satellites for a single baseline. The algorithm of the test method takes into account the linear combination of the weighting coefficients and relates the position errors determined for single baselines. The calculation uses a weighting scheme for three independent baselines denoted as (1A,2A,3A). The proposed research method makes it possible to determine the resultant position errors for ellipsoidal BLh coordinates of the aircraft and significantly improves the accuracy of DGPS positioning. The analysis and evaluation of the new research methodology was checked for data from two flight experiments carried out in Mielec and Dęblin. Based on the calculations performed, it was found that in the flight experiment in Mielec, due to the application of the new research methodology, DGPS positioning accuracy improved from 55 to 94% for all the BLh components. In turn, in the flight experiment in Dęblin, the accuracy of DGPS positioning improved by 63–91%. The study shows that the highest DGPS positioning accuracy is seen when using weighting criterion II, the inverse of the square of the vector length error.
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Prasanna, Gutta Lakshmi, Bodapati Veera Durga Rao, Alugubelli Gopi Reddy, Mandava V. Basaveswara Rao und Manojit Pal. „Lemon Juice Mediated Reaction under Ultrasound Irradiation: Synthesis of Indolofuroquinoxalines as Potential Anticancer Agents“. Mini-Reviews in Medicinal Chemistry 19, Nr. 8 (23.04.2019): 671–78. http://dx.doi.org/10.2174/1389557518666181029100044.
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Background: A non-hazardous synthetic methodology has been developed for the preparation of compounds based on indolofuroquinoxaline framework. Lemon juice that is known to play the role of a biocatalyst in various organic reactions was used for this purpose. Method: A number of indolofuroquinoxaline derivatives were prepared via the lemon juice mediated condensation of methyl 2-(2-chloro-1H-indol-3-yl)-2-oxoacetate or its N-alkyl derivatives with 1,2- diamines under ultrasound irradiation. All the synthesized compounds were screened via an MTT assay for their potential anticancer properties in vitro using a number of cancer cell lines including MDA-MB 231, and MCF7, K562, Colo-205 and IMR-32 and the non-cancerous HEK293 cell line. Compounds 3a, 3b and 3c showed promising growth inhibition against K562, MDA-MB 231 and MCF7 cell lines but no significant effects on HEK293 cell line suggesting their selectivity towards cancer cells. Results and Conclusion: Moreover, according to their IC50 values, all these compounds appeared to be relatively more potent towards K562 cell line over MDA-MB 231 and MCF7 cell lines indicating their potential against leukemia.
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Manoharan, Dhineshkumar, Kannan Kulanthai, Gnanavel Sadhasivam, Vijayan Raji und Paalvannan Thayumanavan. „Synthesis, characterization and evaluation of antidiabetic activity of novel indoline derivatives“. Bangladesh Journal of Pharmacology 12, Nr. 2 (20.05.2017): 20. http://dx.doi.org/10.3329/bjp.v12i2.30872.
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<p class="Abstract">Series of indoline derivatives were synthesized using N-(4-aminophenyl)indoline-1-carbothiamide as a precursor. The confirmation of synthesized compounds was done by <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, LC-MS (ESI) and FT-IR. In vitro antidiabetic activity of synthesized indoline derivatives were examined by standard α-amylase inhibition assay. The compounds 4a (IC<sub>50 </sub>= 52.1 µg/mL) and 4b (IC<sub>50 </sub>= 57.7 µg/mL) showed potent α-amylase inhibition activity. The compounds 3a (IC<sub>50 </sub>= 62.2 µg/mL) and 3b (IC<sub>50 </sub>= 60.7 µg/mL) showed moderate antidiabetic activity.</p><p class="Abstract"><strong>Video Clip of Methodology</strong>:</p><p class="Abstract">19 min 21 sec <a href="https://www.youtube.com/v/k5WdfpM-E8U">Full Screen</a> <a href="https://www.youtube.com/watch?v=k5WdfpM-E8U">Alternate</a></p>
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Luers, Patrick. „Spinal Alteration of Motion Segment Integrity“. Guides Newsletter 12, Nr. 2 (01.03.2007): 1–3. http://dx.doi.org/10.1001/amaguidesnewsletters.2007.marapr01.
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Abstract The Diagnosis-related estimate (DRE) method is the principal methodology to evaluate spinal impairment, and alteration of motion segment integrity results at least in a DRE Category IV rating, based on a single-level fusion. Multilevel fusions are rated using the range-of-motion (ROM) method. Detailed examination of the medical literature identifies definitions of loss of motion segment integrity that differ from those in the AMA Guides to the Evaluation of Permanent Impairment, (AMA Guides), Fourth and Fifth Editions. Evaluators should note that the descriptions of certain figures were revised in the Errata to the Fifth Edition of the AMA Guides. Evaluators should note three key points from the AMA Guides: permanent impairment is based on findings at maximal medical improvement (MMI); motion in the spite must be abnormal to qualify for permanent impairment; and imaging results, by themselves, cannot be used to establish a DRE impairment rating. Overall, evaluators should consider flexion/extension radiographs that are technically adequate and taken at MMI; read and understand the Errata for Figures 15-3a, 15-3b, and 15-3c; and apply only normal translation and angular motion thresholds that are consistent with the scientific literature.
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Carramiñana, Victor, Ana M. Ochoa de Retana, Francisco Palacios und Jesús M. de los Santos. „Synthesis and Antiproliferative Activity of Phosphorus Substituted 4-Cyanooxazolines, 2-Aminocyanooxazolines, 2-Iminocyanooxazolidines and 2-Aminocyanothiazolines by Rearrangement of Cyanoaziridines“. Molecules 26, Nr. 14 (14.07.2021): 4265. http://dx.doi.org/10.3390/molecules26144265.
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Several phosphorus-substituted N-acylated cyanoaziridines 2 and N-carbamoylated cyanoziridines 5 were prepared in good to high yields. N-Acylated cyanoaziridines 2 were used, after ring expansion, in an efficient synthesis of oxazoline derivative 3a and in a completely regio-controlled reaction in the presence of NaI. Conversely, N-carbamoyl cyanoaziridines 5 reacted with NaI to obtain a regioisomeric mixture of 2-aminocyanooxazolines 7. Mild acidic conditions can be used for the isomerization of N-thiocarbamoyl cyanoaziridine 6a into a 2-aminocyanothiazoline derivative 8a by using BF3·OEt2 as a Lewis acid. Likewise, a one pot reaction of NH-cyanoaziridines 1 with isocyanates obtained 2-iminocyanooxazolidines 9 regioselectively. This synthetic methodology involves the addition of isocyanates to starting cyanoaziridines to obtain N-carbamoyl cyanoaziridines 5, which after the ring opening, reacts with a second equivalent of isocyanate to give the final 2-imino cyanooxazolidines 9. In addition, the cytotoxic effect on the cell lines derived from human lung adenocarcinoma (A549) was also screened. 2-Iminooxazolidines 9 exhibited moderate activity against the A549 cell line in vitro. Furthermore, a selectivity towards cancer cells (A549) over non-malignant cells (MCR-5) was detected.
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Prasad, Malavattu G., Chapala V. Lakshmi, Naresh K. Katari, Krishnan Anand, Manojit Pal und Sreekantha B. Jonnalagadda. „Synthesis of 2-Substituted 4-Arylidene-5(4H)-oxazolones as Potential Cytotoxic Agents in the Presence of Lemon Juice as a Biocatalyst“. Combinatorial Chemistry & High Throughput Screening 22, Nr. 9 (01.01.2020): 625–34. http://dx.doi.org/10.2174/1386207322666191024105150.
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Background: The oxazolone class of compounds is known to exert a profound effect on malignant cell proliferation, tumor angiogenesis and /or on the established neoplastic vasculature. Additionally, these compounds are generally known to have a low tendency to interact with DNA which is not common with most of the conventional cytotoxic agents. Thus, this class of compounds is of particular interest for the discovery and development of patient-friendly anticancer agents. Objective: The initial objective of this study was to synthesize and evaluate 2-substituted 4-arylidene- 5(4H)-oxazolones for their potential anticancer properties. Methods: A simple, mild and non-hazardous synthetic methodology has been developed for the preparation of 2-substituted 4-arylidene-5(4H)-oxazolones. The methodology involved lemon juice mediated condensation of N-acyl glycine derivatives including hippuric acid with arylaldehydes in PEG-400 under ultrasound irradiation. All the synthesized compounds were screened via an MTT assay for their potential cytotoxic properties in vitro using the cancerous cell lines e.g. K562 (human chronic myeloid leukemia), Colo-205 (human colon carcinoma), and A549 (human lung carcinoma) and a non-cancerous HEK293 (human embryonic kidney) cell line. Results: Compounds 3a, 3c and 3i showed promising growth inhibition against A549 cell line but no significant effects on HEK293 cell line, indicating their selectivity towards cancer cells. Moreover, their IC50 values suggested that all these compounds were comparable to the reference drug doxorubicin indicating their potential against lung cancer. Conclusion: he 4-arylidene-5(4H)-oxazolone framework presented here could be a new template for the design and discovery of potential anticancer agents especially for lung cancer.
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Snijkers, Frans M. M., Marcel D. Snel, J. F. C. Cooymans, Steven Mullens, A. A. Kodentsov, G. de With und Jan Luyten. „Near-Net-Shape Ceramics by Reactive Processing“. Advances in Science and Technology 45 (Oktober 2006): 701–10. http://dx.doi.org/10.4028/www.scientific.net/ast.45.701.
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Since conventional production of high-temperature materials involves high investments and costly consumption of both energy and time, reaction engineering methodology combined with near-net shaping is often the answer to problems associated with the fabrication of advanced materials. Over the last decades, the number of different reaction–based processing methods for near-net-shaped ceramics has gradually increased. In this review, different reactive processing techniques and their potential for near-netshaping are treated, e.g. SHTS (self-supporting high temperature synthesis), the Lanxide method DIMEX®, reaction bonding (RB), reactive processing of Alumina-Aluminide Alloys (3A) and Al2O3-Al alloyed metal composites (3AMC). In addition to their potential for near-net shaping, other advantages to reactive processing routes are recognized to be reduced processing temperatures, reduced glassy phase formation at the grain boundaries, fine grained microstructures and improved mechanical strength. Since the exothermic reactions constitute the base for reactive processing of high quality materials in an economic way, control of these reactions is essential. The process flows are described together with characteristic features of process and materials. In addition, specific aspects of reaction-based synthesis will be illustrated with examples from own work in the area of reaction bonding of silicon nitride and alumina.
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Li, Yaokuang, Li Ling, Juan Wu und Peng Li. „Who is more likely to become business angels?“ Journal of Entrepreneurship in Emerging Economies 6, Nr. 1 (25.02.2014): 4–20. http://dx.doi.org/10.1108/jeee-06-2013-0017.
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Purpose – The paper is aimed to obtain a clear understanding of influence factors that can increase the possibility to be business angels (BA). Design/methodology/approach – This study develops the 3A model in the Chinese context to design questionnaire, and 334 questionnaires are obtained via focus group sample and targeted snowball approach, and the multinomial logit analysis is used to test a serious of hypotheses. Findings – The paper confirmed that the entrepreneurial experience and wealth are determinants of investment for potential BA, and the wealth have both directly and indirectly positive influence on investment activity through risk preference, namely that richer people prefer risk which impel them to invest as BA. Research limitations/implications – There are two limitations in the paper: first, the macro environment in China has not been taken into consideration in the model; second, the source of the sample focuses on the developed cities in the middle and eastern of China, only reflect the characteristic of angels in these areas, which may somewhat diverges from the reality. Practical implications – The paper would contribute to form the policy which could promote the development of angel investment in China. Originality/value – This paper conducts a preliminary exploration of the factors that have impact on Chinese BA' investment activity based on current research.
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Claeys, Tom, Charles Van Praet, Nicolaas Lumen, Piet Ost, Valérie Fonteyne, Gert De Meerleer, Bieke Lambert et al. „Salvage Pelvic Lymph Node Dissection in Recurrent Prostate Cancer: Surgical and Early Oncological Outcome“. BioMed Research International 2015 (2015): 1–6. http://dx.doi.org/10.1155/2015/198543.
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Methodology. Seventeen patients with prostate-specific antigen (PSA) rise following local treatment for prostate cancer with curative intent underwent open or minimally invasive salvage pelvic lymph node dissection (SLND) for oligometastatic disease (<4 synchronous metastases) or as staging prior to salvage radiotherapy. Biochemical recurrence after complete biochemical response (cBR) was defined as 2 consecutive PSA increases >0,2 ng/mL; and after incomplete biochemical response as 2 consecutive PSA rises. Newly found metastasis on imaging defined clinical progression (CP). Palliative androgen deprivation therapy (ADT) was initiated if >3 metastases were detected or if patients became symptomatic. Kaplan-Meier statistics were applied.Results. Clavien-Dindo grade 1, 2, 3a, and 3b complications were seen in 6, 1, 1, and 2 patients, respectively. Median follow-up time was 22 months. Among 13 patients treated for oligometastatic disease, 8 (67%) had a PSA decline, with 3 patients showing cBR. Median PSA progression-free survival (FS) was 4.1 months and median CP-FS 7 months. Three patients started ADT, resulting in a 2-year ADT-FS rate of 79.5%.Conclusion. SLND is feasible, but postoperative complication rate seems higher than that for primary LND. Biochemical and clinical response duration is limited, but as part of an oligometastatic treatment regime it can defer palliative ADT.
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Ruta, Simona, Camelia Sultana, Cristiana Oprea, Codruta Vagu, Emanoil Ceausu und Costin Cernescu. „HCV non-1b genotypes in injecting drug users from Romania“. Journal of Infection in Developing Countries 10, Nr. 05 (31.05.2016): 523–27. http://dx.doi.org/10.3855/jidc.7019.
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Introduction: Chronic hepatitis C cases diagnosed in Romania were mostly related to unsafe parenteral treatments and blood transfusions; HCV genotype 1b was prevalent. During the last decade, an increasing number of HCV infections was reported among people who inject drugs (PWID). The aim of the current study was to test if this epidemiological shift triggered a diversification of the circulating viral strains. Methodology: HCV genotypes were determined by reverse hybridization in 130 HCV-infected PWID (87.7% males; mean age 27.9 ± 6.7 years, injecting drugs for 8.1 ± 4.8 years). Results: HIV-HCV co-infection was diagnosed in 80.8% of the subjects and 26.9% were HIV-HCV-HBV triple infected. Active HCV viral replication was present in 104 PWID (80%), more frequently in those HIV-co-infected (91.4% vs. 52% in HCV mono-infected, and 77.148.5% in HIV-HCV-HBV triple-infected, p = 0.0001). Non-1b genotypes were prevalent (54.8%), with subtype 1a the most commonly detected (24%), followed by genotypes 3a (14.4%) and 4 (7.7%). Mixed infections with genotypes 1a and 1b were found in nine subjects (8.7%). There was no difference in the genotypes frequencies based on HIV or HBV co-infection status, length of drug usage, or associated risk factors (tattoos, piercing, detention). Conclusion: The continuous surveillance of HCV genotypes in PWID from Romania will add valuable information to the overall European epidemiological picture, with important therapeutic implications.
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Correia, Maria Almira, Sheila Sadeghi und Eduardo Mundo-Paredes. „CYTOCHROME P450 UBIQUITINATION: Branding for the Proteolytic Slaughter?“ Annual Review of Pharmacology and Toxicology 45, Nr. 1 (22.09.2005): 439–64. http://dx.doi.org/10.1146/annurev.pharmtox.45.120403.100127.
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The hepatic cytochromes P450 (P450s) are monotopic endoplasmic reticulum (ER)-anchored hemoproteins engaged in the enzymatic oxidation of a wide variety of endo- and xenobiotics. In the course of these reactions, the enzymes generate reactive O2 species and/or reactive metabolic products that can attack the P450 heme and/or protein moiety and structurally and functionally damage the enzyme. The in vivo conformational unraveling of such a structurally damaged P450 signals its rapid removal via the cellular sanitation system responsible for the proteolytic disposal of structurally aberrant, abnormal, and/or otherwise malformed proteins. A key player in this process is the ubiquitin (Ub)-dependent 26S proteasome system. Accordingly, the structurally deformed P450 protein is first branded for recognition and proteolytic removal by the 26S proteasome with an enzymatically incorporated polyUb tag. P450s of the 3A subfamily such as the major human liver enzyme CYP3A4 are notorious targets for this process, and they represent excellent prototypes for the understanding of integral ER protein ubiquitination. Not all the participants in hepatic CYP3A ubiquitination and subsequent proteolytic degradation have been identified. The following discussion thus addresses the various known and plausible events and/or cellular participants involved in this multienzymatic P450 ubiquitination cascade, on the basis of our current knowledge of other eukaryotic models. In addition, because the detection of ubiquitinated P450s is technically challenging, the critical importance of appropriate methodology is also discussed.
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Hosseinnezhad, Mozhgan, und Kamaladin Gharanjig. „Investigation of photovoltaic properties of nanostructure indoline dye-sensitised solar cells using changes in assembling materials“. Pigment & Resin Technology 46, Nr. 5 (04.09.2017): 393–98. http://dx.doi.org/10.1108/prt-04-2016-0044.
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Purpose The purpose of this paper is to study assembling parameters in dye-sensitised solar cells (DSSCs) performance. For this end, 3a,7a-dihydroxy-5ß-cholanic acid (cheno) are selected as anti-aggregation agent and two solutions, namely, tetrabutyl ammonium iodide and (PMII)IL used as electrolyte. Design/methodology/approach A series of organic dyes were selected using N-substituents carbazole as electron donor group and acrylic acid and cyanoacrylic acid as electron acceptor groups. Absorption properties of purified dyes were studied in solution and on photoelectrode substrate. DSSCs were prepared in the presence of anti-aggregation agent and different electrolyte to determine the photovoltaic performance of each dyes. Findings The results showed that all organic dyes form J-aggregation on the photoanode substrate in the absence of anti-aggregation agent and the amounts of aggregation were reduced in the presence of anti-aggregation agent. DSSCs were fabricated in the presence of anti-aggregation agent. The photovoltaic properties were improved using tetrabutyl ammonium iodide as electrolyte. The maximum power conversion efficiency was achieved for D12 in the presence of cheno and tetrabutyl ammonium iodide as anti-aggregation agent and electrolyte, respectively. Social implications Organic dye attracts more and more attention due to low cost, facile route synthesis and less hazardous. Originality/value The effect of anti-aggregation agent and electrolyte on DSSCs performance was investigated for the first time.
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Blix, Katalin, Károly Pálffy, Viktor Tóth und Torbjørn Eltoft. „Remote Sensing of Water Quality Parameters over Lake Balaton by Using Sentinel-3 OLCI“. Water 10, Nr. 10 (11.10.2018): 1428. http://dx.doi.org/10.3390/w10101428.
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The Ocean and Land Color Instrument (OLCI) onboard Sentinel 3A satellite was launched in February 2016. Level 2 (L2) products have been available for the public since July 2017. OLCI provides the possibility to monitor aquatic environments on 300 m spatial resolution on 9 spectral bands, which allows to retrieve detailed information about the water quality of various type of waters. It has only been a short time since L2 data became accessible, therefore validation of these products from different aquatic environments are required. In this work we study the possibility to use S3 OLCI L2 products to monitor an optically highly complex shallow lake. We test S3 OLCI-derived Chlorophyll-a (Chl-a), Colored Dissolved Organic Matter (CDOM) and Total Suspended Matter (TSM) for complex waters against in situ measurements over Lake Balaton in 2017. In addition, we tested the machine learning Gaussian process regression model, trained locally as a potential candidate to retrieve water quality parameters. We applied the automatic model selection algorithm to select the combination and number of spectral bands for the given water quality parameter to train the Gaussian Process Regression model. Lake Balaton represents different types of aquatic environments (eutrophic, mesotrophic and oligotrophic), hence being able to establish a model to monitor water quality by using S3 OLCI products might allow the generalization of the methodology.
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Nevstad, Kristina, Sjur Børve, Anniken Th Karlsen und Wenche Aarseth. „Understanding how to succeed with project partnering“. International Journal of Managing Projects in Business 11, Nr. 4 (03.09.2018): 1044–65. http://dx.doi.org/10.1108/ijmpb-07-2017-0085.
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Purpose The purpose of this paper is to present new findings to organizations that acknowledge difficulties in implementing and succeeding with project partnering. Design/methodology/approach The investigation is based on a case study where empirical evidence has been collected via semi-structured interviews of 54 professionals within the construction industry. Findings Based on the research the authors were able to identify three main dimensions vital for project partnering success: 1. who related to participant selection; 2. what related to task clarification; and 3. way related to partnering means. These dimensions give rise to what the authors have termed a 3W (Who, What, Way) model on how to succeed with project partnering in practice. The third dimension, way related to partnering means, was found to consist of the four subdimensions: 3a. partnering attitude; 3b. a collaborative culture; 3c. a holistic perspective; and 3d. an accurate handover. Originality/value The authors found 318 papers focusing on partnering, in these only 19 focused on how to succeed with project partnering. The authors have complemented the limited research on how to succeed with project partnering with 54 interviews of professionals. The majority of the existing research has focused on challenges. This paper contributes to the research gap by presenting a 3W model on how to succeed with project partnering.
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Lamquin, Nicolas, Alexis Déru, Sébastien Clerc, Ludovic Bourg und Craig Donlon. „OLCI A/B Tandem Phase Analysis, Part 2: Benefits of Sensors Harmonisation for Level 2 Products“. Remote Sensing 12, Nr. 17 (20.08.2020): 2702. http://dx.doi.org/10.3390/rs12172702.
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This study is a follow-up of a full methodology for the homogenisation and harmonisation of the two Ocean and Land Colour Instrument (OLCI) payloads based on the tandem phase analysis. Sentinel-3B was manoeuvred into a tandem configuration with its operational twin Sentinel-3A already in orbit few weeks after its launch, which was followed by a short drift phase during which Sentinel-3B was progressively moved to a specific orbit phasing of 140° separation from the sentinel-3A. Harmonisation is performed at Level 1 for the radiometric alignment of the OLCI-A TOA radiances to the ones of OLCI-B, considering the slight spectral differences between the two instruments. The benefits of this harmonisation for the main Level 2 products are assessed in the present manuscript for both land and water products. The results validate such benefits showing accuracy between the two sensors after harmonisation better than the products requirements specifications. For the water processing branch, this accuracy opens a path toward an ensemble Sentinel-3 system vicarious calibration with ground-truth measurements. For land products, the tandem phase analysis is also an opportunity to demonstrate that the terrestrial chlorophyll index product requires improvements of the preliminary spectral adjustment of the red-edge channel at 709 nm. As comparisons from the measurements acquired over the tandem phase provides confidence in the alignment of the OLCI-A and OLCI-B series of products, preliminary analysis of the measurements acquired over the drift phase provides the first insights into the sensitivity of the processing algorithms to the geometry of acquisition as well as to calibration residuals of the OLCI field-of-view. As the harmonisation currently performs a radiometric alignment of OLCI-A to OLCI-B, the question of the reference sensor for operational implementation of the harmonisation raises concerns on the individual quality of the calibration of each sensor, notably their across-track consistency. Following the investigations performed at Level 1, where relatively strong calibration residuals are shown between the OLCI cameras and very similarly for both instruments; we discuss the impact of these residuals at L2 using an empirical correction and further conclude with the need to address these problematics with more attention in the future. We conclude with the extreme usefulness of the tandem phase analysis, presently for Level 2 products, and the need to further monitor the temporal stability of the cross-calibration of the OLCI payloads with a view to implementing their harmonisation at operational level.
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Prasad, Malavattu G., Chapala V. Lakshmi, Naresh K. Katari und Manojit Pal. „Lemon Juice as a Biocatalyst Under Ultrasound Irradiation: Synthesis and Pharmacological Evaluation of 2-amino 1,3,4-thiadiazoles“. Anti-Cancer Agents in Medicinal Chemistry 20, Nr. 11 (08.07.2020): 1379–86. http://dx.doi.org/10.2174/1871520620666200409143513.
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Background: The 2-amino 1,3,4-thiadiazole framework has attracted considerable interest because of its prevalence in compounds possessing a wide range of pharmacological properties including anticancer/antitumor activities. Though a number of methods have been reported for the synthesis of this class of compounds, some of them are not straightforward, inexpensive and environmentally friendly. Objective: To synthesize 2-amino-1,3,4-thiadiazole derivatives that could act as potential anticancer agents. Methods: The use of lemon juice as an inexpensive and readily available biocatalyst was explored in the synthesis of 2-amino 1,3,4-thiadiazole derivatives. Accordingly, a convenient method has been developed for the rapid synthesis of this class of compounds under a mild and non-hazardous reaction condition in good yields. The methodology involved the reaction of various acid hydrazides with TMSNCS in the presence of lemon juice in PEG-400 at room temperature (25-30ºC) under ultrasound irradiation. These compounds were assessed for their cytotoxic properties against two different metastatic breast cancer cell lines e.g., MDAMB-231 and MCF-7 and subsequently against SIRT1. Results: The 2-amino 1,3,4-thiadiazole derivatives 3a, 3i, 3j and 3l showed promising growth inhibition of MDAMB- 231 and MCF-7 cell lines and SIRT1 inhibition in vitro. Indeed, 3i was found to be a potent inhibitor of SIRT1. Conclusion: An ultrasound-assisted method facilitated by lemon juice has been developed to synthesize 2-amino- 1,3,4-thiadiazole derivatives that could act as potential anticancer agents.
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Fahim, Qanita, Irfan Ali Mirza, Ayesha Khalid, Anum Imtiaz und Asad Ahmad. „THE HEPATITIS C UNTYPE-ABLE GENOTYPES, AN EMERGENCE OF QUASI-SPECIES IN HCV INFECTED PATIENTS“. PAFMJ 71, Suppl-1 (27.01.2021): S106–12. http://dx.doi.org/10.51253/pafmj.v71isuppl-1.2603.
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Objective: To determine the frequency of Type-able and untype-able genotypes in hepatitis C infected patients,and to observe their association with gender, age, Alanine Aminotranferease and viral load.
Study Design: Cross-sectional analytical study.
Place and Duration of Study: Department of Microbiology, Combined Military Hospital, and Lahore, Pakistanfrom Sep 2017 to Mar 2018.
Methodology: Six hundred forty seven anti HCV antibodies positive serum samples by Enzyme Linked ImmunoSorbant Assay were received from a total of 6791 serum samples. The positive sera were subjected to qualitative PCR and quantitative real time (RT) PCR to determine pre-treatment viral load. Quantitative PCR positive sera with viral load >500IU/ml were further subjected to molecular genotyping by using Ohno et al method.
Result: Out of 647 positive serum samples, type-specific PCR fragments were seen in 424 sera, while 13 (3.1%) of serum samples were of untype-able genotype. In all age groups genotype 3a had emerged as a predominantgenotype 397 (93.6%), followed by 1b 8 (1.9%), 3b 4 (0.9%), 1a 2 (0.5%), while no sample detected to have 2a, 2b,5a, 6a and mixed genotypes. The highest prevalence of untype-ables were seen in 61-70 age group.
Conclusion: Need of the hour is proper sequencing of untype-able genotypes via upgrading existing methodologies. It will not only help the clinicians in achieving sustained virological response but also help in identifying new genotypes/subtypes.
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Quintas-Cardama, Alfonso, Sean M. Post, Kensuke Kojima, Yi Hua Qiu, Michael Andreeff, Carlos E. Bueso-Ramos und Steven M. Kornblau. „High p53 Protein Expression LEVEL Independent Of Mutational Status Is An Adverse Prognostic Factor For Survival In ACUTE Myeloid Leukemia“. Blood 122, Nr. 21 (15.11.2013): 1330. http://dx.doi.org/10.1182/blood.v122.21.1330.1330.
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Abstract Background The tumor suppressor p53 is frequently mutated in human cancer, including acute myeloid leukemia (AML), particularly in cases with high-risk cytogenetics. It has been shown that p53 stabilization, which frequently occurs when the protein is mutated, can compromise its function. We have shown that p53 stabilization, regardless of the presence of mutations, suggesting alterations of other components in the p53 pathway. Methodology p53 expression was determined using high-throughput reverse phase protein array (RPPA) technology in 719 samples from 511 pts. Eleven CD34+ bone marrow (BM) and 10 normal peripheral blood (PB) lymphocyte samples were used as controls. Samples were printed as 5 serial 1:2 dilutions in duplicate using an Aushon 2470 Arrayer. Mutational status of p53 alleles was assessed by Sanger sequencing of exons 5 through 9. Expression of components of the p53 pathway was determined using standard immunohistochemical techniques. Nutlin-3a was used in in vitro culture experiments. Results Paired PB- and BM-derived AML samples expressed similar p53 levels (p=0.25). A trend towards higher p53 expression at relapsed was observed among 47 paired diagnosis/relapse samples (p=0.07). p53 expression correlated directly with CD34 (p=0.001) and inversely correlated with WBC (p=0.007), PB and BM blast burden (p=0.0001), and survival (p=0.01). High p53 (p53high) expression was more associated with unfavorable cytogenetics, particularly -5 (p=0.00001). p53high resulted in lower complete remission (CR) rates (51% vs 56%; p=??), higher relapsed rates (82% vs 62%; p=??), and shorter median overall survival (OS; 29.8 vs. 51 wks, p=0.009) compared to p53low pts. Most cases with p53high had unfavorable cytogenetics. We next correlated p53 stabilization with the presence of p53 mutations in 68 pts. p53 mutations were detected in 20/54 (37%) p53high pts and in 0/14 (0%) pts with p53low. p53high, either in the presence (29 wks) or in the absence (24 wks) of p53 mutations (p=1.0), was associated with significantly shorter OS compared with p53low pts (56 wks; p=0.05). Multivariate analysis revealed p53 expression to be an independent risk factor for survival in AML (p=0.02). p53high was positively correlated with p53pSER15 (p=0.00001), Rbp807p811 (p=0.0002), BAD (p=0.0001), cleaved PARP (p=0.002), and cleaved PARP (p=0.01), and negatively with p21 (p=0.01), and MDM2 (p=0.001).Given the similar OS in p53high pts carrying mutant or wild-type p53, we scored the immunohistochemical expression of MDM2, MDM4, and p21 in 30 p53high pts (9 p53 mutated, 21 wild-type p53). Overexpression of MDM2 was observed in 44% vs 48% pts with mutant vs wild-type p53, respectively, whereas rates were 67% vs 62% for MDM4, and 0% vs 19% for p21, for each respective genotype. Overall, of the 21 p53high pts carrying wild-type p53, 15 (71%) had overexpression of MDM2 and/or MDM4, whereas 81% had no p21 expression, indicating deficient activation of the p53 pathway similar to those cases carrying mutant p53. We are currently assessing response to nutlin-3a therapy in 24 primary AML samples (4 mutant p53, 20 wild-type p53). Results showing the impact of p53 mutation and/or stabilization, and expression levels of MDM2, MDM4, and p21 on nutlin-3a therapy will be presented. Conclusions p53 stabilization (p53high) is a powerful predictive and prognostic factor in AML, which is independent of the presence of mutant p53 alleles. Poor outcomes in pts with p53high lacking p53 mutations are very frequently associated with overexpression of negative regulators of p53 such as MDM2 and/or MDM4 and p21 downregulation, indicating a functionally altered p53 pathway. These findings may have implications for therapies targeting the MDM2/p53 axis in AML. Disclosures: No relevant conflicts of interest to declare.
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Sadeghi, Kaveh, Abbas Ahmadi Vasmehjani, Rasoul Baharlou, Zamaneh Hajikhezri und Seyed Jalal Kiani. „Elevated serum levels of adiponectin and interlukin-28B after IFN/RIB therapy in hepatitis C virus-infected patients“. Journal of Infection in Developing Countries 13, Nr. 05 (31.05.2019): 434–44. http://dx.doi.org/10.3855/jidc.11190.
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Introduction: The interleukin 28B (IL28B) genotype is associated with changes of lipid metabolism in patients infected with hepatitis C virus (HCV). The association of steatosis with serum levels of adiponectin in chronic hepatitis C (CHC) patients has also been documented. This study aimed for the evaluation of serum levels of IL28B and adiponectin as well as the association of IL28B SNPs with different clinicopathological parameters in HCV-infected patients.
Methodology: All 142 HCV-infected patients received peg-interferon plus ribavirin. Detection of rs8099917 and rs12979860 IL-28B genotypes was done with specific primers. Serum IL28 and adiponectin levels were measured using commercial ELISA kits.
Results: Higher levels of both IL28 and adiponectin were found in patients. In Genotype 3a (G3a) -infected patients, IL28 and adiponectin serum levels were significantly higher than those infected with G1a. A correlation was found between increasing levels of AST and ALT in G3a-infected patients and the decrease in IL28 and adiponectin serum levels, respectively, in contrast to G1a-infected patients. Higher levels of both IL28 and adiponectin were associated with both CT allele of rs12979860 and TT allele of rs8099917 in patients in comparison with corresponding alleles in controls.
Conclusions: In contrast to other studies, this study showed higher serum adiponectin levels in HCV-infected patients compared to that in healthy controls. This finding is possibly due to adiponectin resistance caused by down-regulation of adiponectin receptors or tumorigenic effects of adiponectin. Our genotype-based analyses revealed, at least in part, the involvement of the viral factors in the outcome of HCV infection.
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Prasad, Malavattu G., C. Vijaya Lakshmi, Naresh K. Katari, Sreekantha B. Jonnalagadda und Manojit Pal. „Lemon Juice Mediated Synthesis of 3-Substituted Quinazolin-4(3H)-Ones and their Pharmacological Evaluation“. Anti-Cancer Agents in Medicinal Chemistry 19, Nr. 16 (23.01.2020): 2001–9. http://dx.doi.org/10.2174/1871520619666190723151909.
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Background: Compounds containing the quinazoline-4(3H)-one framework constitute an important class of fused N-heterocycles that are found in more than 200 naturally occurring alkaloids. These compounds also show a diverse range of pharmacological activities including antitumor properties. This prompted us to explore a series of quinazolin-4-(3H)-one derivatives having no substituent at C-2 as potential cytotoxic agents. Objective: The objective of this study was to synthesize and evaluate 3-substituted quinazolin-4(3H)-one derivatives for their potential cytotoxic properties. Methods: A convenient method has been developed for the rapid synthesis of this class of compounds under a mild and non-hazardous reaction condition in good yields. The methodology involved a three-component reaction employing isatoic anhydride, amines and glyoxylic acid as reactants in the presence of lemon juice in PEG- 400 at room temperature (25-30ºC) under ultrasound irradiation. All the synthesized compounds were screened via an MTT assay for their potential cytotoxic properties in vitro using the cancerous cell lines e.g. A549, A2780, HepG2, K562, MCF-7 and HCT-116 and a non-cancerous HEK293 cell line. Results: Several compounds such as 3a, 3b, 3d, 3e and 3f showed promising growth inhibition against these cancer cell lines but no significant effects on HEK293 cell line. The IC50 values of these compounds were comparable to doxorubicin whereas 3f significantly induced apoptosis in MCF-7 cells that also was comparable to doxorubicin. Conclusion: An ultrasound-assisted MCR facilitated by lemon juice has been developed to synthesize 3- substituted quinazolin-4(3H)-one derivatives that could act as potential anticancer agents.