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المؤلفHammad, Ayat S.
المؤلفRavindran, Sreenithya
المؤلفKhalil, Ashraf
المؤلفMunusamy, Shankar
تاريخ الإتاحة2017-04-30T05:16:44Z
تاريخ النشر2017-04-10
اسم المنشورCell Stress and Chaperones
المعرّفhttp://dx.doi.org/10.1007/s12192-017-0786-9
الاقتباسAyat S. Hammad, Sreenithya Ravindran, Ashraf Khalil, Shankar Munusamy "Structure–activity relationship of piperine and its synthetic amide analogs for therapeutic potential to prevent experimentally induced ER stress in vitro" Cell Stress and Chaperones (2017) Online: April 10, 2017
الرقم المعياري الدولي للكتاب1355-8145
معرّف المصادر الموحدhttp://hdl.handle.net/10576/5473
الملخصEndoplasmic reticulum (ER) is the key organelle involved in protein folding and maturation. Emerging studies implicate the role of ER stress in the development of chronic kidney disease. Thus, there is an urgent need for compounds that could ameliorate ER stress and prevent CKD. Piperine and its analogs have been reported to exhibit multiple pharmacological activities; however, their efficacy against ER stress in kidney cells has not been studied yet. Hence, the goal of this study was to synthesize amide-substituted piperine analogs and screen them for pharmacological activity to relieve ER stress using an in vitro model of tunicamycin-induced ER stress using normal rat kidney (NRK-52E) cells. Five amide-substituted piperine analogs were synthesized and their chemical structures were elucidated by pertinent spectroscopic techniques. An in vitro model of ER stress was developed using tunicamycin, and the compounds of interest were screened for their effect on cell viability, and the expression of ER chaperone GRP78, the pro-apoptotic ER stress marker CHOP, and apoptotic caspases 3 and 12 (via western blotting). Our findings indicate that exposure to tunicamycin (0.5 μg/mL) for 2 h induces the expression of GRP78 and CHOP, and apoptotic markers (caspase-3 and caspase-12) and causes a significant reduction in renal cell viability. Pre-treatment of cells with piperine and its cyclohexylamino analog decreased the tunicamycin-induced upregulation of GRP78 and CHOP and cell death. Taken together, our findings demonstrate that piperine and its analogs differentially regulate ER stress, and thus represent potential therapeutic agents to treat ER stress-related renal disorders.
راعي المشروعThis study was supported by the intramural grants (QUUG-CPH-CPH-13/14-2; QUST-CPH-SPR-12/13-5; QUSTCPH- FALL-13/14-6; QUST-CPH-SPR-13/14-8; QUST-CPH-FALL-14/15-5; QUST-CPH-SPR-14/15-14) awarded by the Office of Academic Research, Qatar University, Doha, Qatar.
اللغةen
الناشرSpringer Netherlands
الموضوعPiperine
Amide piperine analogs
ER stress
NRK-52E
Tunicamycin
Chronic kidney disease
العنوانStructure–activity relationship of piperine and its synthetic amide analogs for therapeutic potential to prevent experimentally induced ER stress in vitro
النوعArticle
ESSN1466-1268
dc.accessType Abstract Only


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