Journal: Journal of Pharmacy Research

Article Id: JPRS-PC-0000216
Title: Triazolo aspirins inhibit proliferation of C6 glioma cell lines in vitro
Category: Pharmaceutical Chemistry
Section: Research Article
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    Background: 1, 2, 3 triazole based molecules are emerging as promising anticancer drugs. Aspirin inhibits cell proliferation and induces apoptosis in various cancer cell lines. We have synthesized novel conjugates incorporating both aspirin and triazole ring systems. Gliomas are the most devastating intracerebral neoplasms that occur due to transformation of astrocytes. Deregulation of NF-κB signaling pathway adds to the enriched glioma persistence, proliferation and chemo resistance. Hence, the present study was carried out to test the efficacy of these compounds against the growth of C6 glioma cell lines in vitro. Methods: Triazolo aspirins were synthesized by regioselective Cu (I)-catalyzed azide alkyne cycloaddition. The structures of these compounds were characterized by IR, 1HNMR, 13C NMR, mass spectrometric data and micro analysis. The compounds were tested for their efficacy to inhibit the growth of C6 glioma cell lines in vitro. Results: Among the triazolo aspirins investigated, dioxoisoindolin-butyl-triazole (abbreviated as TIBMAB) showed significant activity with IC-50 of 100±60 ìM. The anti-proliferative activity through MTT and Clonogenic assay indicated decreased viability, FACS studies showed cell cycle G2/M-phase arrest, TUNEL studies exhibited that many cells were undergoing apoptotic cell death, immunofluorescence studies displayed ability of TIBMAB to inhibit the TNF-α induced translocation of p65 into nucleus, western blot analysis confirmed TIBMAB induced apoptosis through activation of caspase-3 along with enriched PARP cleavage and inhibited the TNF-α induced translocation of NF-κB into nucleus. Conclusion: TIBMAB showed substantial inhibition of C6 glioma cell line proliferation and decreased cell survival partly by inhibiting the NF-κB signaling.

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    Author(s) Name:

    Anwita Mudiraj1, Khamushavalli Geeviman2, Phanithi Prakash Babu2, A. Ram Reddy1,*

    Affiliation(s) Name:

    1Department of Chemistry, University College of Science, Osmania University, Hyderabad, India-500007
    2Department of Biotechnology, School of Life Sciences, University of Hyderabad, Hyderabad, India- 500046


    *Corresponding author.
    A. Ram Reddy
    Department of Chemistry,
    University College of Science,
    Osmania University, Hyderabad, India-500007

    Received on:21-05-2014; Revised on: 08-06-2014; Accepted on:11-06-2014

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    Author:

    Anwita Mudiraj1, Khamushavalli Geeviman2, Phanithi Prakash Babu2, A. Ram Reddy1,*

    Title:Triazolo aspirins inhibit proliferation of C6 glioma cell lines in vitro
    Journal:Journal of Pharmacy Research
    Vol(issue):8 (June)
    Year:2014
    Page No: (741-750)
  • Experimental Methods Keywords

    Methodology: regioselective Cu (I)-catalyzed azide alkyne cycloaddition,IR, 1HNMR, 13C NMR, mass spectrometric data and micro analysis
    Research Materials:Triazolo aspirins

Keywords

Aspirin Triazole C6 glioma cell line NF-κB signaling.

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