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Synthesis and protective effects of novel salidroside analogues on glucose and serum depletion induced apoptosis in PC12 cells.

Abstract
Salidroside is a natural product isolated from Rhodiola rosea L. which possesses a wide range of biological activities, especially neuroprotective effects in the treatment of ischemic stroke. In an attempt to improve its neuroprotective effects, a series of novel salidroside analogues were synthesized and their neuroprotective activities were evaluated against the glucose and serum depletion-induced cell death in differentiated PC12 cells. Most target compounds displayed protective effects on the cell viability, especially for compound 6, which had a great potency superior to salidroside. MTT assay and Hoechst 33342 staining collectively showed that pretreatment with 6 attenuated cell viability loss and reduced apoptotic death in cultured PC12 cells with glucose and serum depletion. And its neuroprotective effects might be associated with the increase of the apoptosis-related protein Bcl-2/Bax expression ratio, and also with the inhibition of caspase-3 activation. Therefore, our new findings may provide potentially important information for further development of salidroside analogues and lay the basis for further studies on the cerebral ischemic stroke and neurodegenerative diseases for human clinical treatment.
AuthorsYahong Zhao, Yong Ling, Jing Zhao, Ying Yuan, Yibin Guo, Qiong Liu, Bingxin Wu, Zuoyou Ding, Yumin Yang
JournalArchiv der Pharmazie (Arch Pharm (Weinheim)) Vol. 346 Issue 4 Pg. 300-7 (Apr 2013) ISSN: 1521-4184 [Electronic] Germany
PMID23440725 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Chemical References
  • Glucosides
  • Neuroprotective Agents
  • Phenols
  • Proto-Oncogene Proteins c-bcl-2
  • bcl-2-Associated X Protein
  • Caspase 3
  • Glucose
  • rhodioloside
Topics
  • Animals
  • Apoptosis (drug effects)
  • Caspase 3 (metabolism)
  • Cell Survival (drug effects)
  • Glucose (metabolism)
  • Glucosides (chemical synthesis, chemistry, pharmacology)
  • Neuroprotective Agents (chemical synthesis, chemistry, pharmacology)
  • PC12 Cells
  • Phenols (chemical synthesis, chemistry, pharmacology)
  • Proto-Oncogene Proteins c-bcl-2 (genetics)
  • Rats
  • Structure-Activity Relationship
  • bcl-2-Associated X Protein (genetics)

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