Kooperativer Bibliotheksverbund

Berlin Brandenburg

and
and

Your email was sent successfully. Check your inbox.

An error occurred while sending the email. Please try again.

Proceed reservation?

Export
Filter
Language
Year
  • 1
    Language: English
    In: Journal of medicinal chemistry, 09 August 2012, Vol.55(15), pp.6985
    Keywords: Pharmacy, Therapeutics, & Pharmacology ; Chemistry;
    E-ISSN: 1520-4804
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 2
    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
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 3
    Language: English
    In: Cancer Research, 10/01/2014, Vol.74(19 Supplement), pp.1637-1637
    ISSN: 0008-5472
    E-ISSN: 1538-7445
    Source: CrossRef
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 4
    Language: English
    In: Life Sciences, 15 December 2015, Vol.143, pp.147-155
    Description: Aims: The interactions between cancer cells and platelets have been recognized to play an important role in cancer progress as well as metastasis, and interference with cancer–platelet interactions is an attractive strategy for cancer therapy. In the present study, two β-nitrostyrene derivatives: 3, 4-methylene-dioxy-β-nitrostyrene (MNS) and 4-O-benzoyl-3-methoxyl-β-nitrostyrene (BMNS) have been tested for their inhibitory effect on platelet activation caused by metastatic human breast cancer MDA-MB-231 and Hs578T cells. Main methods: Washed human platelets were co-incubated with breast cancer cells, and platelet aggregation was determined turbidimetrically. Platelet adhesion to cancer cells and P-selectin expression were measured by flow cytometry. Platelet-derived growth factor (PDGF) released from cancer cell-stimulated platelets was determined by enzyme-linked immunosorbent assay (ELISA). Key findings: MNS and BMNS prevented cancer cell-induced platelet aggregation, P-selectin expression, and PDGF secretion. Moreover, the β-nitrostyrenes reduced platelet adhesion to cancer cells, suggesting the initial cancer–platelet interactions are inhibited. In contrast to current antiplatelet strategies, the glycoprotein IIb/IIIa (GPIIb/IIIa) antagonist RGDS peptide only prevented cancer cells-induced platelet aggregation, but not platelet adhesion and secretion; whereas the cyclooxygenase inhibitor aspirin and the adenosine diphosphate (ADP) scavenger apyrase affected neither platelet aggregation nor platelet secretion. Significance: The inhibitory effects of the β-nitrostyrene derivatives on cancer–platelet interactions may offer a potential approach for repressing cancer metastasis.
    Keywords: Cancer ; Platelet Aggregation ; Adhesion ; P-Selectin ; Β-Nitrostyrene ; Sciences (General) ; Biology
    ISSN: 0024-3205
    E-ISSN: 1879-0631
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 5
    Language: English
    In: Bioorganic & Medicinal Chemistry, 2010, Vol.18(21), pp.7621-7627
    Description: A series of β-nitrostyrenes were synthesized and subjected to anti-platelet aggregation assay and cytotoxicity assay. Most of them exhibited the most potent inhibitory effects on thrombin- and collagen-induced platelet aggregation. Our previous studies demonstrated that two cytotoxic β-nitrostyrene derivatives, 3,4-methylenedioxy-β-nitrostyrene (MNS) and 4- -benzoyl-3-methoxy-β-nitrostyrene (BMNS) exhibit potent anti-platelet activities. In this study, a series of β-nitrostyrenes were synthesized and subjected to anti-platelet aggregation assay and cytotoxicity assay. The mono- and di-substitutions on the B ring of BMNS tended to increase the anti-platelet activity and decrease the cytotoxic activity. Of these, compounds and exhibited the most potent inhibitory effects on thrombin- and collagen-induced platelet aggregation (IC ⩽ 0.7 μM) without significant cytotoxicity on a human cancer cell line (up to 20 μM). Further studies indicated that compounds and inhibited platelet aggregation via prevention of glycoprotein IIb/IIIa activation. The potent and novel effects of BMNS derivatives make them attractive candidates for the development of new anti-platelet agents.
    Keywords: Anti-Platelet Aggregation ; Cytotoxicity ; Β-Nitrostyrenes ; Structure–Activity Relationships (SAR) ; Medicine ; Chemistry ; Anatomy & Physiology
    ISSN: 0968-0896
    E-ISSN: 1464-3391
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 6
    Language: English
    In: Tetrahedron, 04 March 2014, Vol.70(9), pp.1800-1804
    Description: A four-component Ugi reaction (Ugi-4CR) utilizing formylphenyl boronic acids under mild condition was developed for the synthesis of arylboronic acid analogs. The reactions were performed in methanol and accelerated by microwave irradiation, which makes this strategy suitable for constructing boronic-containing chemical libraries. Two of the synthesized analogs were found to have cytotoxic activity against HepG2, MDA-MB231, and A549 cancer cell lines, demonstrating the potential application of this approach in developing novel boron-containing pharmaceuticals. In this study, an Ugi four-component reaction (Ugi-4CR) utilizing unprotected boronic acid building blocks under mild condition is developed. The described reactions were performed in methanol and accelerated by employing microwave irradiation. This strategy allows the direct generation of boronic acid analogs without protection and deprotection operations of boronic acid moiety, making it suitable for the preparation of boron-containing chemical libraries. The synthesized boronic acid analogs were subsequently evaluated for their cytotoxic activity by the MTT assay. Two potential lead compounds were found to be cytotoxic against HepG2, MDA-MB231, and A549 cancer cell lines, demonstrating the potential application of this approach in developing novel boron-containing pharmaceuticals.
    Keywords: Boronic Acids ; Ugi-4cr ; Multicomponent Reaction ; Microwave-Assisted Synthesis ; Acid/Base Extraction ; Chemistry
    ISSN: 0040-4020
    E-ISSN: 1464-5416
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 7
    Language: English
    In: European Journal of Pharmacology, 2006, Vol.546(1), pp.142-147
    Description: Thrombin activates human platelets through proteolytic activation of two protease-activated receptors (PARs), PAR1 and PAR4. In the present study, we show that, RWJ-56110, a potent synthetic PAR1 antagonist, inhibited platelet aggregation caused by a low concentration (0.05 U/ml) of thrombin, but lost its effectiveness when higher concentrations of thrombin were used as stimulators. YD-3, a non-peptide PAR4 antagonist, alone had little or no effect on thrombin-induced platelet aggregation, significantly enhanced the anti-aggregatory activity of PAR1 antagonist. In addition, we demonstrate for the first time that P-selectin expression in thrombin-stimulated platelets can be synergistically prevented by combined treatment of PAR1 antagonist and PAR4 antagonist. These results indicate that thrombin-induced platelet activation cannot be effectively inhibited by just blocking either single thrombin receptor pathway, and suggest a rationale for potential combination therapy in arterial thrombosis.
    Keywords: Protease-Activated Receptor ; Thrombin ; Platelet Activation ; Pharmacy, Therapeutics, & Pharmacology
    ISSN: 0014-2999
    E-ISSN: 1879-0712
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 8
    Language: English
    In: Nurse Education Today, 2011, Vol.31(8), pp.768-773
    Description: There are increasing opportunities for nurses to engage in continuing learning via the Internet; hence, it is important to explore nurses' attitudes toward web-based continuing learning. This paper explores 267 Taiwanese clinical nurses' attitudes toward web-based continuing learning. In addition, the role of the nurses' Internet self-efficacy in their attitudes is investigated. This study utilizes two questionnaires to respectively survey the nurses' Internet self-efficacy and their attitudes toward web-based continuing learning. In particular, the Internet Self-efficacy Survey includes two scales: ‘Basic self-efficacy’ (the perceived confidence of using basic Internet functions, such as the confidence in using a web browser or searching for online information) and ‘Advanced self-efficacy’ (the perceived confidence of using advanced Internet functions, such as the confidence in online discussion or making online payments). Exploratory factor analyses indicated adequate reliability and validity of the two questionnaires. The regression analyses revealed that both nurses' basic and advanced Internet self-efficacy can positively explain the perceived usefulness, ease of use and friendly feeling when using web-based continuing learning environments, whereas nurses' advanced Internet self-efficacy was the only predictor to explain how they intend to use web-based continuing learning environments more.
    Keywords: Internet Self-Efficacy ; Internet Attitude ; Web-Based Continuing Learning ; Medicine ; Nursing
    ISSN: 0260-6917
    E-ISSN: 1532-2793
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 9
    Language: English
    In: Science Education, September 2005, Vol.89(5), pp.822-846
    Description: The main purpose of this study was to explore the effects of long‐term constructivist‐oriented science instruction on elementary school students' process of constructing cognitive structures. Furthermore, such effects on different science achievers were also investigated. The subjects of this study were 69 fifth graders in Taiwan, while they were assigned to either a constructivist‐oriented instruction group or a traditional teaching group. The research treatment was conducted for 5 months, including six instructional units, and students' cognitive structures were probed through interviews coupled with a “metalistening technique'' after the instruction of each unit. The interview narratives were transcribed into the format of “flow maps.” In addition, the information processing modes shown in the flow maps were also investigated through a series of content analyses. The findings showed that the students in the constructivist‐oriented instruction group attained significantly better learning outcomes in terms of the extent and integration of their cognitive structures, metacognition engagement, and the usage of information processing strategies. Moreover, it was also revealed that both high achievers and low achievers benefited from the constructivist‐oriented instructional activities, but in different ways. For example, both high achievers and low achievers in the constructivist‐oriented instruction group attained better usage of information processing strategies than their counterparts in traditional teaching group did; but only high achievers displayed better usage of higher order information processing modes (i.e., inferring or explaining) than their counterparts in traditional teaching group did. The results in this study finally suggest a four‐stage model for students' process of constructing cognitive structure under the constructivist‐oriented science instruction, including “cognitive structure acquisition,” “metacognition enrichment,” “cognitive structure integration,” and “cognitive structure refinement.” © 2005 Wiley Periodicals, Inc. 822–846, 2005
    Keywords: Education ; Sciences (General);
    ISSN: 0036-8326
    E-ISSN: 1098-237X
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 10
    Language: English
    In: Food Chemistry, 01 September 2013, Vol.140(1-2), pp.305-314
    Description: roots showed oestrogenic and anti-platelet activities. ► Twenty-six compounds were isolated and divided into 10 different skeletons. ► The biosynthetic pathway of the isolated dihydrobenzofuroisocoumarins was proposed. can be used to develop nutritional dietary supplements. The ethanolic extract of (Liliaceae) roots showed potential oestrogenic and anti-platelet activities. Twenty-six compounds were isolated and classified as 10 skeletons, including two unusual new dihydrobenzofuroisocoumarins, (+)-platyphyllarin A ( ) and B ( ), one new butanoate, ethyltributanoate ( ), and two new homoisoflavanones, (−)-liriopein A ( ) and B ( ), along with 21 known compounds, including six homoisoflavonoids, one chalcone, six amides, one lignan, one fatty acid derivative, one alkaloid, three benzenoids, and two steroids. The biosynthetic pathway of compounds and was proposed in the current investigation. The oestrogenic activity of the isolates was evaluated utilising the pER8:GUS reporter assay system in transgenic plant as well as the SEAP reporter assay system in MCF-7 breast cancer cell-line; the anti-platelet activity was evaluated using the anti-platelet aggregation assay. Several components exhibited significant oestrogenic and anti-platelet activities; demonstrating for the first time the potential use of as a nutritional supplement for cardiovascular and endocrine diseases.
    Keywords: Liriope Platyphylla ; Dihydrobenzofuroisocoumarin ; Homoisoflavonoid ; Oestrogenic Activity ; Anti-Platelet Effect ; Arabidopsis Per8:Gus Reporter Assay ; Chemistry ; Diet & Clinical Nutrition ; Economics
    ISSN: 0308-8146
    E-ISSN: 1873-7072
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
Close ⊗
This website uses cookies and the analysis tool Matomo. Further information can be found on the KOBV privacy pages