• English
    • العربية
  • العربية
  • Login
  • QU
  • QU Library
  •  Home
  • Communities & Collections
  • Help
    • Item Submission
    • Publisher policies
    • User guides
    • FAQs
  • About QSpace
    • Vision & Mission
View Item 
  •   Qatar University Digital Hub
  • Qatar University Institutional Repository
  • Academic
  • Faculty Contributions
  • College of Pharmacy
  • Pharmacy Research
  • View Item
  • Qatar University Digital Hub
  • Qatar University Institutional Repository
  • Academic
  • Faculty Contributions
  • College of Pharmacy
  • Pharmacy Research
  • View Item
  •      
  •  
    JavaScript is disabled for your browser. Some features of this site may not work without it.

    Synthesis And Pharmacological Screening Of Novel Piperine Analogs For Potential In Vitro Protection From Endoplasmic Reticulum Stress

    Thumbnail
    View/Open
    qfarc.2014.HBSP0714.pdf (99.18Kb)
    Date
    2016
    Author
    Samir Hammad, Ayat
    Munusamy, Shankar
    Khalil, Ashraf
    Metadata
    Show full item record
    Abstract
    Background: The endoplasmic reticulum (ER) is the chief organelle involved in protein homeostasis. Perturbations to the ER protein folding machinery caused by hyperlipidemia, hyperglycemia or hypoglycemia has been shown to trigger ER stress and activate the unfolded protein response (UPR) as a defense mechanism. Accumulating evidences implicate the role of ER stress in the development of chronic kidney disease. Thus there is an urgent need for novel compounds, which have the ability to ameliorate ER stress to treat or prevent any organ damage. Among the natural compounds, piperine and its analogs have been reported to exhibit multiple pharmacological activities, however, the efficacy of piperine and its analogs against ER stress in kidney cells is still unknown. Thus, the goal of the current study is to synthesize a range of piperine analogs and screen them for pharmacological activity to relieve ER stress using an in vitro model of tunicamycin-induced ER stress in rat renal proximal tubular (NRK-52E) cells. Methods: To perform a structure-activity relationship study, several piperine analogs were prepared using piperic acid as a starting material. The structures of the obtained compounds were confirmed by liquid chromatography-mass spectrometry (LC/MS), differential scanning calorimetry (DSC), fourier transform infrared (FT-IR) and nuclear magnetic resonance (NMR). The in vitro ER stress model was developed using tunicamycin. Results: Several piperine analogs were synthesized and their structures were elucidated. The preliminary findings indicate that exposure to tunicamycin induces the expression of ER chaperone GRP 78 in NRK-52E cells. The MTT assay confirms the reduction in cell viability even with a low concentration of 1 ug/mL of tunicamycin for 15 minutes. The developed in vitro model will be used to evaluate the effect of piperine analogs on ER stress markers. Conclusion: The synthesis, structural elucidation and the results of the preliminary screening of selected piperine analogs will be presented.
    URI
    https://doi.org/10.5339/qfarc.2014.HBSP0714
    DOI/handle
    http://hdl.handle.net/10576/30189
    Collections
    • Pharmacy Research [‎1399‎ items ]

    entitlement


    Qatar University Digital Hub is a digital collection operated and maintained by the Qatar University Library and supported by the ITS department

    Contact Us | Send Feedback
    Contact Us | Send Feedback | QU

     

     

    Home

    Submit your QU affiliated work

    Browse

    All of Digital Hub
      Communities & Collections Publication Date Author Title Subject Type Language Publisher
    This Collection
      Publication Date Author Title Subject Type Language Publisher

    My Account

    Login

    Statistics

    View Usage Statistics

    About QSpace

    Vision & Mission

    Help

    Item Submission Publisher policiesUser guides FAQs

    Qatar University Digital Hub is a digital collection operated and maintained by the Qatar University Library and supported by the ITS department

    Contact Us | Send Feedback
    Contact Us | Send Feedback | QU

     

     

    Video