Document Detail

CPU86017, a berberine derivative, attenuates cardiac failure through normalizing calcium leakage and downregulated phospholamban and exerting antioxidant activity.
MedLine Citation:
PMID:  20139899     Owner:  NLM     Status:  MEDLINE    
AIM: To investigate whether CPU86017, a berberine derivative, attenuates heart failure by blocking calcium influx and exerting its antioxidant activity.
METHODS: Myocardial infarction was induced in male Sprague-Dawley rats for 17 d followed by isoproterenol (ISO) (5 mg/kg, sc) treatment for 5 d to reduce cardiac function. The rats were divided into 5 groups: sham operation, myocardial infarction (MI), MI plus ISO, and co-treated (in mg/kg, po) with either propranolol (PRO, 10) or CPU86017 (80). Hemodynamic measurements were conducted, and measurements of the redox system, calcium handling proteins and endothelin (ET) system in vivo were done. Furthermore, calcium flux studies and PLB immunocytochemistry were conducted in vitro.
RESULTS: Compared to sham operation, HF was evident following MI and further worsened by ISO treatment. This occurred in parallel with downregulated mRNA and protein production of SERCA2a, PLB, and FKBP12.6, and was associated with upregulation of preproET-1, endothelin converting enzyme, and PKA mRNA production in the myocardium in vivo. Calcium leakage was induced by ISO treatment of isolated beating myocytes in vitro. These changes were attenuated by treatment with either PRO or CPU86017. PLB fluorescence in myocytes was downregulated by ISO treatment, and was relieved significantly by treatment with antioxidant aminoguanidine, ascorbic acid or CPU86017 in vitro.
CONCLUSION: HF, calcium leakage, downregulated PLB, FKBP12.6, SERCA2a production, and upregulated PKA were caused by ISO treatment, and were abolished by CPU86017 treatment. The beneficial effects of CPU86017 are attributable to its antioxidant and calcium influx blocking effects.
Min-you Qi; Yu Feng; De-zai Dai; Na Li; Yu-si Cheng; Yin Dai
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Acta pharmacologica Sinica     Volume:  31     ISSN:  1745-7254     ISO Abbreviation:  Acta Pharmacol. Sin.     Publication Date:  2010 Feb 
Date Detail:
Created Date:  2010-02-08     Completed Date:  2010-04-29     Revised Date:  2014-09-20    
Medline Journal Info:
Nlm Unique ID:  100956087     Medline TA:  Acta Pharmacol Sin     Country:  United States    
Other Details:
Languages:  eng     Pagination:  165-74     Citation Subset:  IM    
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MeSH Terms
Antioxidants / pharmacology*
Base Sequence
Berberine / analogs & derivatives*,  pharmacology
Calcium / metabolism*
Calcium-Binding Proteins / metabolism*
DNA Primers
Heart Failure / prevention & control*
Oxidative Stress
Rats, Sprague-Dawley
Reverse Transcriptase Polymerase Chain Reaction
Reg. No./Substance:
0/4-chlorobenzyltetrahydroberberine; 0/Antioxidants; 0/Calcium-Binding Proteins; 0/DNA Primers; 0/phospholamban; 0I8Y3P32UF/Berberine; SY7Q814VUP/Calcium

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