Synthesis and preliminary evaluation of neuroprotection of celastrol analogues in PC12 cells.
A series of celastrol analogues were synthesized, and their neuroprotective effect against t-BHP-induced cytotoxicity was investigated in neuronal PC12 cells. Their effects on Hsp70 protein expression were quantified by Western blot analysis. The study found that compound CL12 is more effective than the parent celastrol against t-BHP-induced cytotoxicity. CL12 up-regulates Hsp70 protein expression dose-dependently. These results suggest that CL12 is a potential candidate for the intervention of neurodegenerative diseases.
Sun
Hongli
H
Institute of New Drug Research, Jinan University College of Pharmacy, Guangzhou, China.
Xu
Lipeng
L
Yu
Pei
P
Jiang
Jie
J
Zhang
Gaoxiao
G
Wang
Yuqiang
Y
D000818:Animals; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D018840:HSP70 Heat-Shock Proteins / Q000096:biosynthesis; D008968:Molecular Conformation; D018696:Neuroprotective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D016716:PC12 Cells; D053978:Pentacyclic Triterpenes; D051381:Rats; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020122:tert-Butylhydroperoxide / Q000037:antagonists & inhibitors / Q000494:pharmacology
D018840:HSP70 Heat-Shock Proteins; D018696:Neuroprotective Agents; D053978:Pentacyclic Triterpenes; D014315:Triterpenes; D020122:tert-Butylhydroperoxide; C050414:celastrol