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Berlin Brandenburg

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  • 1
    Language: English
    In: PLoS ONE, 2012, Vol.7(5), p.e37764
    Description: Withanolides are a large group of steroidal lactones found in Solanaceae plants that exhibit potential anticancer activities. We have previously demonstrated that a withanolide, tubocapsenolide A, induced cycle arrest and apoptosis in human breast cancer cells, which was associated with the inhibition of heat shock protein 90 (Hsp90). To investigate whether other withanolides are also capable of inhibiting Hsp90 and to analyze the structure-activity relationships, nine withanolides with different structural properties were tested in human breast cancer cells MDA-MB-231 and MCF-7 in the present study. Our data show that the 2,3-unsaturated double bond-containing withanolides inhibited Hsp90 function, as evidenced by selective depletion of Hsp90 client proteins and induction of Hsp70. The inhibitory effect of the withanolides on Hsp90 chaperone activity was further confirmed using in vivo heat shock luciferase activity recovery assays. Importantly, Hsp90 inhibition by the withanolides was correlated with their ability to induce cancer cell death. In addition, the withanolides reduced constitutive NF-κB activation by depleting IκB kinase complex (IKK) through inhibition of Hsp90. In estrogen receptor (ER)-positive MCF-7 cells, the withanolides also reduced the expression of ER, and this may be partly due to Hsp90 inhibition. Taken together, our results suggest that Hsp90 inhibition is a general feature of cytotoxic withanolides and plays an important role in their anticancer activity.
    Keywords: Research Article ; Biology ; Medicine ; Molecular Biology ; Cell Biology ; Oncology ; Biochemistry
    E-ISSN: 1932-6203
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  • 2
    Language: English
    In: PLoS ONE, 01 January 2015, Vol.10(10), p.e0141184
    Description: In this study, six 2-phenylnaphthalenes with hydroxyl groups were synthesized in high yields by the demethylation of the corresponding methoxy-2-phenylnaphthalenes, and one 2-phenylnaphthalene with an amino group was obtained by hydrogenation. All of the 2-phenylnaphthalene derivatives were...
    Keywords: Sciences (General)
    E-ISSN: 1932-6203
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  • 3
    Language: English
    In: PLoS ONE, 2012, Vol. 7(5), p. e37897
    Description: In a structure-activity relationship (SAR) study, 3-methoxy-1,4-phenanthrenequinones, calanquinone A (6a), denbinobin (6b), 5-OAc-calanquinone A (7a) and 5-OAc-denbinobin (7b), have significantly promising cytotoxicity against various human cancer cell lines (IC50 0.08-1.66 mu g/mL). Moreover, we also established a superior pharmacophore model for cytotoxicity (r = 0.931) containing three hydrogen bond acceptors (HBA1, HBA2 and HBA3) and one hydrophobic feature (HYD) against MCF-7 breast cancer cell line. The pharmacophore model indicates that HBA3 is an essential feature for the oxygen atom of 5-OH in 6a-b and for the carbonyl group of 5-OCOCH3 in 7a-b, important for their cytotoxic properties. The SAR for moderately active 5a-b (5-OCH3), and highly active 6a-b and 7a-b, are also elaborated in a spatial aspect model. Further rational design and synthesis of new cytotoxic phenanthrene analogs can be implemented via this model. Additionally, employing a ChemGPS-NP based model for cytotoxicity mode of action (MOA) provides support for a preliminary classification of compounds 6a-b as topoisomerase II inhibitors.
    Keywords: Medical And Health Sciences ; Medicin Och Hälsovetenskap
    ISSN: 1932-6203
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  • 4
    Language: English
    In: PLoS ONE, 01 January 2014, Vol.9(10), p.e111365
    Description: Neutrophil activation is associated with the development of organ injury after trauma-hemorrhagic shock. In the present study, ursolic acid inhibited the superoxide anion generation and elastase release in human neutrophils. Administration of ursolic acid attenuated trauma-hemorrhagic shock-induced...
    Keywords: Sciences (General)
    ISSN: 09680896
    E-ISSN: 1932-6203
    E-ISSN: 14643391
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  • 5
    Language: English
    In: Antimicrobial Agents and Chemotherapy, 2011, Vol. 55(3), p.1021
    Description: 1,2,3,4,6-Penta-O-galloyl-β-D-glucopyranose (PGG) is an active ingredient in plants that are commonly used in Chinese medicine to treat inflammation. We demonstrate here that PGG, at 6.25 μM, does not inhibit the growth of Staphylococcus aureus, and yet it prevents biofilm formation on polystyrene and polycarbonate surfaces. At the same concentration, PGG is not toxic to human epithelial and fibroblast cells. PGG has an IB₅₀ value, i.e., the PGG concentration that inhibits 50% biofilm formation, of 3.6 μM. The value is substantially lower than that of N-acetylcysteine, iodoacetamide, and N-phenyl maleimide, which are known to inhibit biofilm formation by S. aureus. Biochemical and scanning electron microscopy results also reveal that PGG inhibits initial attachment of the bacteria to solid surface and the synthesis of polysaccharide intercellular adhesin, explaining how PGG inhibits biofilm formation. The results of this study demonstrate that coating PGG on polystyrene and silicon rubber surfaces with polyaniline prevents biofilm formation, indicating that PGG is highly promising for clinical use in preventing biofilm formation by S. aureus.
    Keywords: Anti-Bacterial Agents -- Pharmacology ; Biofilms -- Drug Effects ; Hydrolyzable Tannins -- Pharmacology ; Staphylococcus Aureus -- Drug Effects;
    ISSN: 0066-4804
    ISSN: 00664804
    E-ISSN: 10986596
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  • 6
    Language: English
    In: Psychological Reports, April 2012, Vol.110(2), pp.416-426
    Description: The purpose of the study was to examine the relations of five dimensions of free-time management (including goal setting and evaluating, technique, values, immediate response, and scheduling) with leisure boredom, and whether these factors could predict leisure boredom. A total of 500 undergraduates from a university in southern Taiwan were surveyed with 403 usable questionnaires was returned. Pearson correlation analysis revealed that five dimensions of free-time management had significant negative relationships with leisure boredom. Furthermore, the results of stepwise regression analysis revealed that four dimensions of free-time management were significant contributors to leisure boredom. Finally, we suggested students can avoid boredom by properly planning and organizing leisure time and applying techniques for managing leisure time.
    Keywords: Psychology
    ISSN: 0033-2941
    E-ISSN: 1558-691X
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  • 7
    Language: English
    In: PLoS ONE, 01 January 2011, Vol.6(8), p.e23922
    Description: Protoapigenone, a natural flavonoid possessing an unusual p-quinol moiety on its B-ring, is a novel prospective anticancer agent with low toxicity that is currently in development. The first economical, one-step synthesis of protoapigenone from...
    Keywords: Sciences (General)
    E-ISSN: 1932-6203
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  • 8
    Language: English
    In: Angewandte Chemie International Edition, 16 August 2011, Vol.50(34), pp.7885-7891
    Description: : NMR spectroscopy and isothermal titration calorimetry show that calcium ions are chelated by the hydroxylated THF ring of acetogenins, which results in formation of complexes that aid the Ca cations in penetrating cell membranes and in elevating the intracellular calcium level (see picture). This disruption of intracellular calcium homeostasis induces mitochondrial depolarization and mediates cell toxicity.
    Keywords: Acetogenins ; Calcium ; Chelates ; Cytotoxicity ; Isothermal Titration Calorimetry
    ISSN: 1433-7851
    E-ISSN: 1521-3773
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  • 9
    Language: English
    In: Phytochemistry, August 2016, Vol.128, pp.60-70
    Description: Phytochemical study of the methanolic root extract of allowed for the characterization of 18 non-alkaloid terpenoids. Their structures have skeletons composed of six rearranged -podocarpanes, 11 -podocarpanes, and a 3,4- -30- -friedelane. These were characterized based on 2D NMR, IR, UV, and MS spectroscopic analysis and their absolute configurations were determined by single-crystal X-ray studies, as well as by H NMR spectroscopic analysis for the corresponding chiral derivatives. The isolates were evaluated for therapeutic potential against hepatitis C virus (HCV) infection to human hepatoma Huh7.5 cells. Terpenoids with anti-HCV activity were identified from . The 9(10 → 20)- -podocarpanes were reported from this genus for the first time. The amide coupling reaction on 3,4- -30- -friedelane yielded unexpected compounds.
    Keywords: Flueggea Virosa ; Euphorbiaceae ; Anti-Hepatitis C Virus ; Ent-Podocarpane ; 3,4-Seco-30-nor-Friedelane ; Botany
    ISSN: 0031-9422
    E-ISSN: 1873-3700
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  • 10
    Language: English
    In: Journal of agricultural and food chemistry, 27 April 2011, Vol.59(8), pp.4288-93
    Description: We evaluated the possible anticancer performance of a natural compound, goniothalamin (GTN), against human lung cancer using as a non-small cell lung cancer (NSCLC) cell line, H1299, as the model system. Cellular proliferation was significantly inhibited by GTN. Using an improved alkaline comet-nuclear extract (comet-NE) assay, GTN was found to induce a significant increase in the tail DNA. Wound healing and zymography assays showed that GTN attenuated cell migration and caused a reduction in the activity level of two major migration-associated matrix metalloproteinases, MMP-2 and MMP-9. It can be concluded that the DNA-damaging effect of GTN against lung cancer cells leads to growth inhibition as well as a depression in migration ability. Therefore, GTN has potential as a chemotherapeutic agent against lung cancer.
    Keywords: Apoptosis -- Drug Effects ; Carcinoma, Non-Small-Cell Lung -- Pathology ; Cell Division -- Drug Effects ; Cell Movement -- Drug Effects ; DNA Damage -- Drug Effects ; Lung Neoplasms -- Pathology ; Pyrones -- Pharmacology
    ISSN: 00218561
    E-ISSN: 1520-5118
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