title: Short- and long-term effects of xuezhikang, an extract of cholestin, on serum proprotein convertase subtilisin/kexin type 9 levels.
abstract: OBJECTIVE
  To investigate the short- and long-term effects of Xuezhikang (XZK), an extract of cholestin, on proprotein convertase subtilisin/kexin type 9 (PCSK9) level.
  
  
  METHODS
  Thirty rats were randomly divided into three groups and were given saline, XZK 1,200 mg/kg or lovastatin 10 mg/kg respectively by daily gavage for 3 days (n=10 for each). Sixteen patients without previous lipid-lowering drug treatment for dyslipidemia received XZK 1,200 mg daily for 8 weeks. Fasting blood samples and liver tissue were collected at day 3 for rats, while the blood samples were obtained at baseline and week 8 from patients. The serum PCSK9 and lipid profile were measured. The expression of hepatic low density lipoprotein (LDL) receptor and sterol regulatory element binding protein 2 (SREBP-2) were measured by real time-PCR.
  
  
  RESULTS
  PCSK9 levels in rats were significantly increased in the XZK and lovastatin groups (P=0.002, P=0.003 vs. control) at day 3, while no significant differences were found in the levels of lipid parameters. PCSK9 levels in patients increased by 34% (P=0.006 vs. baseline) accompanied by total cholesterol and LDL-cholesterol decreased by 22% and 28% P=0.001, P=0.002 vs. baseline). The hepatic mRNA levels of LDL-receptor and SREBP-2 were significantly increased in the XZK and lovastatin groups.
  
  
  CONCLUSIONS
  XZK has significant impact on PCSK9 in a short- and long-term manner in both rats and humans. Moreover, the data indicated that as lovastatin, XZK increased PCSK9 levels through SREBP-2 pathway.
authors.affiliation: Division of Dyslipidemia, State Key Laboratory of Cardiovascular Disease, Fuwai Hospital, National Center for Cardiovascular Disease, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100037, China.
authors.forename: Yan-jun
authors.initials: YJ
authors.lastname: Jia
authors.affiliation: Division of Dyslipidemia, State Key Laboratory of Cardiovascular Disease, Fuwai Hospital, National Center for Cardiovascular Disease, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100037, China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: Division of Dyslipidemia, State Key Laboratory of Cardiovascular Disease, Fuwai Hospital, National Center for Cardiovascular Disease, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100037, China.
authors.forename: Jun
authors.initials: J
authors.lastname: Liu
authors.affiliation: Division of Dyslipidemia, State Key Laboratory of Cardiovascular Disease, Fuwai Hospital, National Center for Cardiovascular Disease, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100037, China.
authors.forename: Yuan-lin
authors.initials: YL
authors.lastname: Guo
authors.affiliation: Division of Dyslipidemia, State Key Laboratory of Cardiovascular Disease, Fuwai Hospital, National Center for Cardiovascular Disease, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100037, China.
authors.forename: Rui-xia
authors.initials: RX
authors.lastname: Xu
authors.affiliation: Division of Dyslipidemia, State Key Laboratory of Cardiovascular Disease, Fuwai Hospital, National Center for Cardiovascular Disease, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100037, China. lijianjun938@yahoo.com.
authors.forename: Jian-jun
authors.initials: JJ
authors.lastname: Li
mesh_terms: D000818:Animals; D001688:Biological Products / Q000737:chemistry*; D004365:Drugs, Chinese Herbal / Q000494:pharmacology*; D005260:Female; D006801:Humans; D008055:Lipids / Q000097:blood; D008297:Male; D008875:Middle Aged; D000071449:Proprotein Convertase 9 / Q000097:blood*; D017207:Rats, Sprague-Dawley; D011973:Receptors, LDL / Q000235:genetics / Q000378:metabolism; D051782:Sterol Regulatory Element Binding Protein 2 / Q000235:genetics / Q000378:metabolism; D013997:Time Factors
chemical_list: D001688:Biological Products; D004365:Drugs, Chinese Herbal; D008055:Lipids; D011973:Receptors, LDL; D051782:Sterol Regulatory Element Binding Protein 2; C117343:red yeast rice; C496822:xuezhikang; C472125:PCSK9 protein, human; C510804:PCSK9 protein, rat; D000071449:Proprotein Convertase 9
keywords: Chinese medicine; Xuezhikang; lipid profile; proprotein convertase subtilisin/kexin type 9; statin