title: Cardioprotective effects of baicalein on heart failure via modulation of Ca(2+) handling proteins in vivo and in vitro.
abstract: OBJECTIVE
  Baicalein is a widely used Chinese herbal medicine extracted from Labiatae plants Scutellaria baicalensis Georgi's dry root, which has multiple pharmacological activities. However, the precise mechanism of baicalein against myocardial remodeling remains poorly understood. The aim of our study was to investigate the underlying mechanism of baicalein treatment in rats model of heart failure (HF) and rat myocardial cells (H9C2).
  
  
  METHODS
  HF model was established by abdominal aorta constriction in rats and incubation with 50μM isoproterenol for 48h in H9C2 cells. Various molecular biological experiments were performed to assess the effects of baicalein on cardiac function, myocardial remodeling, apoptosis and Ca(2+) handling proteins.
  
  
  RESULTS
  In the present study, first we found that baicalein alleviated HF in vivo. Additionally, treatment with baicalein inhibited the myocardial fibrosis, restrained the expression and activity of MMP2 and MMP9, and suppressed apoptosis in heart tissue. Moreover, baicalein could inhibit the cardiac myocyte hypertrophy and apoptosis induced by isoproterenol in vitro. Finally we found that baicalein could modulate the expressions and activities of Ca(2+) handling proteins, including downregulation of phosphorylation of Ca(2+)/calmodulin-dependent protein kinase II (CaMKII) and expression of Na(+)/Ca(2+)-exchangers (NCX1), upregulation of sarcoplasmic reticulum Ca(2+) ATPase 2 (SERCA2) and ryanodine receptor 2 (RYR2). Baicalein also restrained the decreased SERCA activity induced by aortic banding.
  
  
  CONCLUSIONS
  Our studies suggested that baicalein alleviated myocardial remodeling and improved cardiac function via modulation of Ca(2+) handling proteins, which may be a potential phytochemical flavonoid for therapeutics of HF.
authors.affiliation: Department of Cardiology, The First Affiliated Hospital of Harbin Medical University, Harbin 150001, People's Republic of China.
authors.forename: Fali
authors.initials: F
authors.lastname: Zhao
authors.affiliation: Department of Cardiology, The First Affiliated Hospital of Harbin Medical University, Harbin 150001, People's Republic of China. Electronic address: fulu320@126.com.
authors.forename: Lu
authors.initials: L
authors.lastname: Fu
authors.affiliation: Department of Laboratory Medicine, The First Affiliated Hospital of Harbin Medical University, Harbin 150001, People's Republic of China.
authors.forename: Wei
authors.initials: W
authors.lastname: Yang
authors.affiliation: Department of Cardiology, The First Affiliated Hospital of Harbin Medical University, Harbin 150001, People's Republic of China.
authors.forename: Yuhui
authors.initials: Y
authors.lastname: Dong
authors.affiliation: Department of Cardiology, The First Affiliated Hospital of Harbin Medical University, Harbin 150001, People's Republic of China.
authors.forename: Jing
authors.initials: J
authors.lastname: Yang
authors.affiliation: Department of Ophthalmology, The First Affiliated Hospital of Harbin Medical University, Harbin 150001, People's Republic of China.
authors.forename: Shoubin
authors.initials: S
authors.lastname: Sun
authors.affiliation: Department of Cardiology, The First Affiliated Hospital of Harbin Medical University, Harbin 150001, People's Republic of China.
authors.forename: Yuling
authors.initials: Y
authors.lastname: Hou
mesh_terms: D000818:Animals; D017209:Apoptosis / Q000187:drug effects; D002316:Cardiotonic Agents / Q000737:chemistry / Q000627:therapeutic use*; D002460:Cell Line; D005355:Fibrosis; D044950:Flavanones / Q000737:chemistry / Q000627:therapeutic use*; D006321:Heart / Q000187:drug effects* / Q000503:physiopathology*; D006333:Heart Failure / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology / Q000503:physiopathology*; D008297:Male; D009206:Myocardium / Q000378:metabolism / Q000473:pathology; D051381:Rats; D017207:Rats, Sprague-Dawley; D031364:Scutellaria baicalensis / Q000737:chemistry
chemical_list: D002316:Cardiotonic Agents; D044950:Flavanones; C006680:baicalein
keywords: Apoptosis; Baicalein; Ca(2+) handling proteins; Heart failure (HF); Myocardial remodeling