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https://www.readbyqxmd.com/read/28641157/design-synthesis-and-structure-activity-relationship-studies-of-a-novel-focused-library-of-2-3-4-substituted-oxazolidines-with-antiproliferative-activity-against-cancer-cell-lines
#1
Saulo F Andrade, Bárbara G Oliveira, Larissa C Pereira, Jonas P Ramos, Angélica R Joaquim, Martin Steppe, Elaine M Souza-Fagundes, Ricardo J Alves
In the present work we describe the synthesis and antiproliferative evaluation of a focused library of 30 novel oxazolidines designed by modification of N-substituent, by ring variation, by alkyl variation or by extension of the structure. It was noted that carbamate and N,O-aminal groups were essential for activity. In general, replacement of the phenyl ring with pyridinyl was not tolerated. However, the introduction of a second phenyl ring with an appropriate spacer at the 3- or 4-position of the first phenyl ring generally enhanced the cytotoxic profile...
June 12, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28636040/tamoxifen-like-metallocifens-target-the-thioredoxin-system-determining-mitochondrial-impairment-leading-to-apoptosis-in-jurkat-cells
#2
Valeria Scalcon, Michèle Salmain, Alessandra Folda, Siden Top, Pascal Pigeon, Hui Zhi Shirley Lee, Gérard Jaouen, Alberto Bindoli, Anne Vessières, Maria Pia Rigobello
Tamoxifen-like metallocifens (TLMs) of the group-8 metals (Fe, Ru, and Os) show strong anti-proliferative activity on cancer cell lines resistant to apoptosis, owing to their unique redox properties. In contrast, the thioredoxin system, which is involved in cellular redox balance, is often overexpressed in cancer cells, especially in tumour types resistant to standard chemotherapies. Therefore, we investigated the effect of these three TLMs on the thioredoxin system and evaluated the input of the metallocene unit in comparison with structurally related organic tamoxifens...
June 21, 2017: Metallomics: Integrated Biometal Science
https://www.readbyqxmd.com/read/28634298/analyses-of-pde-regulated-phosphoproteomes-reveal-unique-and-specific-camp-signaling-modules-in-t-cells
#3
Michael-Claude G Beltejar, Ho-Tak Lau, Martin G Golkowski, Shao-En Ong, Joseph A Beavo
Specific functions for different cyclic nucleotide phosphodiesterases (PDEs) have not yet been identified in most cell types. Conventional approaches to study PDE function typically rely on measurements of global cAMP, general increases in cAMP-dependent protein kinase (PKA), or the activity of exchange protein activated by cAMP (EPAC). Although newer approaches using subcellularly targeted FRET reporter sensors have helped define more compartmentalized regulation of cAMP, PKA, and EPAC, they have limited ability to link this regulation to downstream effector molecules and biological functions...
June 20, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28631525/polyphenol-profile-by-uhplc-ms-ms-anti-glycation-antioxidant-and-cytotoxic-activities-of-several-samples-of-propolis-from-the-northeastern-semi-arid-region-of-brazil
#4
Jadriane de Almeida Xavier, Iara Barros Valentim, Fabiana O S Camatari, Alberto M M de Almeida, Henrique Fonseca Goulart, Jamylle Nunes de Souza Ferro, Emiliano de Oliveira Barreto, Bruno Coelho Cavalcanti, Carla B G Bottoli, Marília Oliveira Fonseca Goulart
CONTEXT: Propolis has promising biological activities. Propolis samples from the Northeast of Bahia, Brazil - sample A from Ribeira do Pombal and B, from Tucano - were investigated, with new information regarding their biological activities. OBJECTIVE: This paper describes the chemical profile, antioxidant, anti-glycation and cytotoxic activities of these propolis samples. MATERIAL AND METHODS: Ethanol extracts of these propolis samples (EEP) and their fractions were analyzed to determine total phenolic content (TPC); antioxidant capacity through DPPH(•), FRAP and lipid peroxidation; anti-glycation activity, by an in vitro glucose (10 mg/mL) bovine serum albumine (1 mg/mL) assay, during 7 d; cytotoxic activity on cancer (SF295, HCT-116, OVCAR-8, MDA-MB435, MX-1, MCF7, HL60, JURKAT, MOLT-4, K562, PC3, DU145) and normal cell lines (V79) at 0...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28618355/chemical-constituents-from-the-fruits-of-ligustrum-japonicum-and-their-inhibitory-effects-on-t-cell-activation
#5
Quynh-Mai Thi Ngo, Hyun-Su Lee, Van Thu Nguyen, Jeong Ah Kim, Mi Hee Woo, Byung Sun Min
A previously undescribed nor-dammarane, 3β,20,23-trihydroxy-24,25,26,27-tetranordammarane; three previously undescribed secoiridoid glycosides, ligujaponosides A-B, and iso-oleonuzhenide; and twenty three known compounds, were isolated from the fruits of Ligustrum japonicum Thunb. Their chemical structures were elucidated by extensive spectroscopic analyses, including 1D and 2D NMR, and HRMS. The isolated compounds were screened for immunosuppressive effects on T activated cells by evaluating interleukin-2 (IL-2) production...
June 12, 2017: Phytochemistry
https://www.readbyqxmd.com/read/28610775/cytotoxic-effect-of-a-novel-naphthylchalcone-against-multiple-cancer-cells-focusing-on-hematologic-malignancies
#6
Mariana Franzoni Maioral, Camila do Nascimento Bodack, Natália Marceli Stefanes, Álisson Bigolin, Alessandra Mascarello, Louise Domeneghini Chiaradia-Delatorre, Rosendo Augusto Yunes, Ricardo José Nunes, Maria Cláudia Santos-Silva
Chalcones are natural compounds described in the literature by its several properties including cytotoxic activity against several tumor types. Considering that the search for new chemotherapeutic agents is still necessary, the aim of this study was to investigate the cytotoxic mechanisms involved in cell death induced by a synthetic chalcone (A23) on different tumor cells. Chalcone A23 reduced the cell viability of twelve tumor cell lines in a concentration and time dependent manner and it was more cytotoxic against acute leukemia cells...
June 10, 2017: Biochimie
https://www.readbyqxmd.com/read/28609193/dna-methylome-profiling-on-the-infinium-humanmethylation450-array-from-limiting-quantities-of-genomic-dna-from-a-single-small-archived-bloodspot
#7
Kripa Asrani, Gary M Shaw, Jasper Rine, Nicholas J Marini
AIMS: Archived newborn bloodspots are valuable sample collections for genetic and epigenetic disease research. However, they have often been stored for long periods of time, under less than ideal circumstances, and nucleic acid yields can be low, particularly when samples become limiting. We wished to determine whether the quantity and quality of genomic DNA (gDNA) isolated from a single, surgical bloodspot punch (2 mm dia.) were adequate for accurate and reliable DNA methylome profiling on the Illumina HumanMethylation450 array...
June 13, 2017: Genetic Testing and Molecular Biomarkers
https://www.readbyqxmd.com/read/28606226/-expression-of-%C3%AE-integrin-family-members-in-children-with-t-cell-acute-lymphoblastic-leukemia
#8
Qing-Lin Kong, Xi-Zhou An, Xian-Min Guan, Yi-Mei Ma, Peng-Fei Li, Shao-Yan Liang, Yan-Ni Hu, Ying-Hui Cui, Jie Yu
OBJECTIVE: To study the expression of β-integrin family members in children with T-cell acute lymphoblastic leukemia (T-ALL) and their significance. METHODS: Quantitative real-time PCR analyses were performed to assess the expression levels of β-integrin family members in bone marrow samples from 22 children with newly-diagnosed T-ALL and 21 controls (16 children with non-malignant hematologic disease and 5 healthy donors with bone marrow transplantation). Jurkat cells were treated with integrin inhibitor arginine-glycine-aspartate (Arg-Gly-Asp, RGD) peptide...
June 2017: Zhongguo Dang Dai Er Ke za Zhi, Chinese Journal of Contemporary Pediatrics
https://www.readbyqxmd.com/read/28604752/tumor-cell-derived-lactate-induces-taz-dependent-upregulation-of-pd-l1-through-gpr81-in-human-lung-cancer-cells
#9
J Feng, H Yang, Y Zhang, H Wei, Z Zhu, B Zhu, M Yang, W Cao, L Wang, Z Wu
The clinical success of immunotherapy that inhibits the negative immune regulatory pathway programmed cell death protein 1/PD-1 ligand (PD-1/PD-L1) has initiated a new era in the treatment of metastatic cancer. PD-L1 expression is upregulated in many solid tumors including lung cancer and functions predominantly in lactate-enriched tumor microenvironments. Here, we provided evidence for PD-L1 induction in response to lactate stimulation in lung cancer cells. Lactate-induced PD-L1 induction was mediated by its receptor GPR81...
June 12, 2017: Oncogene
https://www.readbyqxmd.com/read/28597878/incorporation-studies-of-clickable-ceramides-in-jurkat-cell-plasma-membranes
#10
T Walter, J Schlegel, A Burgert, A Kurz, J Seibel, M Sauer
The incorporation properties of ceramide analogues for click chemistry in Jurkat T cells were investigated. The analogues varied in the acyl chain length and the position of the functional group for click chemistry. Fluorescence microscopy studies including anisotropy and quenching experiments showed significant differences in the accessibility of the functional group indicating different incorporation properties into the plasma membrane.
June 9, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28596482/aging-dependent-dna-hypermethylation-and-gene-expression-of-gstm1-involved-in-t-cell-differentiation
#11
Shu-Hui Yeh, Cheng-Ling Liu, Ren-Chieh Chang, Chih-Chiang Wu, Chia-Hsueh Lin, Kuender D Yang
This study investigated whether aging was associated with epigenetic changes of DNA hypermethylation on immune gene expression and lymphocyte differentiation. We screened CG sites of methylation in blood leukocytes from different age populations, picked up genes with age-related increase of CG methylation content more than 15%, and validated immune related genes with CG hypermethylation involved in lymphocyte differentiation in the aged population. We found that 12 genes (EXHX1、 IL-10、 TSP50、 GSTM1、SLC5A5、SPI1、F2R、LMO2、PTPN6、FGFR2、MMP9、MET) were associated with promoter or exon one DNA hypermethylation in the aged group...
May 23, 2017: Oncotarget
https://www.readbyqxmd.com/read/28593141/glycosyl-chains-and-25-hydroxycholesterol-contribute-to-the-intracellular-transport-of-amyloid-beta-a%C3%AE-42-in-jurkat-t-cells
#12
Neha Sharma, KeangOK Baek, Huong T T Phan, Naofumi Shimokawa, Masahiro Takagi
Amyloid beta (Aβ) is a peptide responsible for the development of Alzheimer's disease (AD). Misfolding and accumulation of endogenous Aβ can lead to neural cell apoptosis through endoplasmic reticulum (ER) stress. Added exogenous Aβ can also result in ER stress, leading to neurotoxicity and apoptosis, which is identical to that caused by the endogenous peptide. We have speculated that the endocytic transport of Aβ causes ER stress and have previously shown that the oxysterol, in particular, 7-ketocholesterol (7-keto) induces more surface interaction between Aβ-42 and Jurkat cells than cholesterol...
June 2017: FEBS Open Bio
https://www.readbyqxmd.com/read/28584192/arf6-and-rab22-mediate-t-cell-conjugate-formation-by-regulating-clathrin-independent-endosomal-membrane-trafficking
#13
Debra L Johnson, Jessica Wayt, Jean M Wilson, Julie G Donaldson
Endosomal trafficking can influence the composition of the plasma membrane and the ability of cells to polarize their membranes. Here we examined whether trafficking through clathrin-independent endocytosis (CIE) affects the ability of T cells to form a cell-cell conjugate with antigen presenting cells (APCs). We show that CIE occurs in both the Jurkat T cell line and primary human T cells. In Jurkat cells, the activities of two guanine nucleotide binding proteins, Arf6 and Rab22, influence CIE and conjugate formation...
June 5, 2017: Journal of Cell Science
https://www.readbyqxmd.com/read/28582973/a-novel-anti-cd22-scfv-apoptin-fusion-protein-induces-apoptosis-in-malignant-b-cells
#14
Solmaz Agha Amiri, Soraya Shahhosseini, Najmeh Zarei, Dorsa Khorasanizadeh, Elahe Aminollahi, Faegheh Rezaie, Mehryar Zargari, Mohammad Azizi, Vahid Khalaj
CD22 marker is a highly internalizing antigen which is located on the surface of B-cells and is being used as a promising target for treatment of B cell malignancies. Monoclonal antibodies targeting CD22 have been introduced and some are currently under investigation in clinical trials. Building on the success of antibody drug conjugates, we developed a fusion protein consisting of a novel anti-CD22 scFv and apoptin and tested binding and therapeutic effects in lymphoma cells. The recombinant protein was expressed in E...
December 2017: AMB Express
https://www.readbyqxmd.com/read/28578326/targeting-jurkat-t-lymphocyte-leukemia-cells-by-an-engineered-interferon-alpha-hybrid-molecule
#15
Dehai Yu, Zhonghua Du, Wei Li, Huaqiu Chen, Songgen Ye, Andrew R Hoffman, Jiuwei Cui, Ji-Fan Hu
BACKGROUND/AIMS: Adult T-cell leukemia/lymphoma (ATL) is a very aggressive T cell malignancy that carries a poor prognosis, primarily due to its resistance to chemotherapy and to life-threatening infectious complications. Interferon-alpha (IFNα) has been used in combination with the anti-retroviral drug zidovudine to treat patients with ATL. However, the efficacy of long-term therapy is significantly limited due to the systemic toxicity of IFNα. METHODS: We utilized phage display library screening to identify short peptides that specifically bind to Jurkat T lymphocyte leukemia cells...
June 5, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28576978/hox5-paralogous-genes-modulate-th2-cell-function-during-chronic-allergic-inflammation-via-regulation-of-gata3
#16
Catherine Ptaschinski, Steven M Hrycaj, Matthew A Schaller, Deneen M Wellik, Nicholas W Lukacs
Allergic asthma is a significant health burden in western countries, and continues to increase in prevalence. Th2 cells contribute to the development of disease through release of the cytokines IL-4, IL-5, and IL-13, resulting in increased airway eosinophils and mucus hypersecretion. The molecular mechanisms behind the disease pathology remain largely unknown. In this study we investigated a potential regulatory role for the Hox5 gene family, Hoxa5, Hoxb5, and Hoxc5, genes known to be important in lung development within mesenchymal cell populations...
June 2, 2017: Journal of Immunology: Official Journal of the American Association of Immunologists
https://www.readbyqxmd.com/read/28573252/induction-of-cell-cycle-arrest-and-apoptosis-by-ormenis-eriolepis-a-morrocan-endemic-plant-in-various-human-cancer-cell-lines
#17
Lamiae Belayachi, Clara Aceves-Luquero, Nawel Merghoub, Silvia Fernández de Mattos, Saaîd Amzazi, Priam Villalonga, Youssef Bakri
BACKGROUND: Ormenis eriolepis Coss (Asteraceae) is an endemic Moroccan subspecies, traditionally named "Hellala" or "Fergoga". It's usually used for its hypoglycemic effect as well as for the treatment of stomacal pain. As far as we know, there is no scientific exploration of anti tumoral activity of Ormenis eriolepis extracts. MATERIALS AND METHODS: In this regard, we performed a screening of organic extracts and fractions in a panel of both hematological and solid cancer cell lines, to evaluate the potential in vitro anti tumoral activity and to elucidate the respective mechanisms that may be responsible for growth arrest and cell death induction...
2017: African Journal of Traditional, Complementary, and Alternative Medicines: AJTCAM
https://www.readbyqxmd.com/read/28571538/high-throughput-screening-assay-to-identify-modulators-of-il-17-expression
#18
Mohamed Boudjelal, Ana Maria Ruiz-Avendano, Gonzalo Colmenarejo, Sergio A Senar-Sancho, Ashley Barnes, Stephen A Harrison
Herein we demonstrate the successful development of a new RORt-enhanced IL-17F promoter-luciferase reporter assay and its use in a parallel high throughput screening approach, alongside a RORt TR-FRET assay, to rapidly identify new small molecule RORt/IL-17 inhibitors and evaluate their mode of action. We sought to identify cell-permeable small-molecule inhibitors of RORt for rapid progression into hit-to-lead chemistry. As such, we developed the IL-17F promoter luciferase reporter assay in a stable human T-cell (Jurkat) line expressing the RORt receptor and miniaturised it to a final volume of 8 μL in 1536 well plates for HTS use in screening a library of > 350k compounds...
June 1, 2017: Combinatorial Chemistry & High Throughput Screening
https://www.readbyqxmd.com/read/28566684/quantitative-refractive-index-distribution-of-single-cell-by-combining-phase-shifting-interferometry-and-afm-imaging
#19
Qinnan Zhang, Liyun Zhong, Ping Tang, Yingjie Yuan, Shengde Liu, Jindong Tian, Xiaoxu Lu
Cell refractive index, an intrinsic optical parameter, is closely correlated with the intracellular mass and concentration. By combining optical phase-shifting interferometry (PSI) and atomic force microscope (AFM) imaging, we constructed a label free, non-invasive and quantitative refractive index of single cell measurement system, in which the accurate phase map of single cell was retrieved with PSI technique and the cell morphology with nanoscale resolution was achieved with AFM imaging. Based on the proposed AFM/PSI system, we achieved quantitative refractive index distributions of single red blood cell and Jurkat cell, respectively...
May 31, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28565807/arsenic-trioxide-increases-expression-of-secreted-frizzled-related-protein-1-gene-and-inhibits-the-wnt-%C3%AE-catenin-signaling-pathway-in-jurkat-cells
#20
Yan Wang, Zunsong Wang, Hong Li, Wenwei Xu, Lin Dong, Yan Guo, Saran Feng, Kehong Bi, Chuansheng Zhu
The aim of the present study was to investigate the demethylation effect of arsenic trioxide (As2O3) on the secreted frizzled-related protein 1 (SFRP1) gene and its ability to inhibit the Wingless-type MMTV integration site family (WNT) pathway in Jurkat cells. Methylation-specific polymerase chain reaction was used to examine the CpG island methylation status of the SFRP1 gene in leukemia cell lines. In addition, the effects on Jurkat cells of treatment with different concentrations of As2O3 for 48 h were investigated...
May 2017: Experimental and Therapeutic Medicine
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