title: 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.
authors: Jiangsu Key Laboratory of Neuroregeneration, Department of Pharmacy, School of Medical, Nantong University, Nantong, PR China.
authors: Yahong
authors: Y
authors: Zhao
authors: Yong
authors: Y
authors: Ling
authors: Jing
authors: J
authors: Zhao
authors: Ying
authors: Y
authors: Yuan
authors: Yibin
authors: Y
authors: Guo
authors: Qiong
authors: Q
authors: Liu
authors: Bingxin
authors: B
authors: Wu
authors: Zuoyou
authors: Z
authors: Ding
authors: Yumin
authors: Y
authors: Yang
mesh_terms: D000818:Animals; D017209:Apoptosis / Q000187:drug effects*; D053148:Caspase 3 / Q000378:metabolism; D002470:Cell Survival / Q000187:drug effects*; D005947:Glucose / Q000378:metabolism; D005960:Glucosides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D018696:Neuroprotective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D016716:PC12 Cells; D010636:Phenols / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000235:genetics; D051381:Rats; D013329:Structure-Activity Relationship; D051028:bcl-2-Associated X Protein / Q000235:genetics
chemical_list: D005960:Glucosides; D018696:Neuroprotective Agents; D010636:Phenols; D019253:Proto-Oncogene Proteins c-bcl-2; D051028:bcl-2-Associated X Protein; D053148:Caspase 3; D005947:Glucose; C009172:rhodioloside