title: The hemostatic effect study of Cirsium setosum on regulating α1-ARs via mediating norepinephrine synthesis by enzyme catalysis.
abstract: BACKGROUND
  Cirsium setosum (CS) is the aboveground part of Cephalanoplos segetum Kitam. Although it has been used as a hemostatic treatment for thousands of years and is still in use today, the mechanism of CS on regulating ARs is still not clear.
  
  
  OBJECTIVE
  In this study, we aimed to clarify the mechanism of CS on regulating ARs.
  
  
  METHODS
  We developed a simple method based on UPLC/Q-TOF MS combined adrenergic receptor dual-luciferase reporter assay systems for the rapid determination of active constituents in CS. The mechanism of tyramine, the main active component for regulating ARs, was further investigated by an in vitro norepinephrine biotransformation test and in vivo vaso activity tests.
  
  
  RESULTS
  Two phenethylamine ARs regulators (tyramine and N-methyltyramine) in CS were characterized, and it was found that tyramine could induce vasoconstriction via regulation of α1-ARs by mediating norepinephrine synthesis.
  
  
  CONCLUSIONS
  The hemostatic effect of CS is associated with tyramine and N-methyltyramine, via regulation of α1-ARs, and the mechanism of tyramine is related to mediating norepinephrine synthesis by enzyme catalysis.
authors.affiliation: Tianjin University of Traditional Chinese Medicine, Tianjin 300193, People's Republic of China.
authors.forename: Nianwei
authors.initials: N
authors.lastname: Chang
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Haihe Education Park, 38 Tongyan Road, Tianjin 300353, People's Republic of China.
authors.forename: Yanmei
authors.initials: Y
authors.lastname: Li
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Haihe Education Park, 38 Tongyan Road, Tianjin 300353, People's Republic of China.
authors.forename: Mengge
authors.initials: M
authors.lastname: Zhou
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Haihe Education Park, 38 Tongyan Road, Tianjin 300353, People's Republic of China.
authors.forename: Jie
authors.initials: J
authors.lastname: Gao
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Haihe Education Park, 38 Tongyan Road, Tianjin 300353, People's Republic of China.
authors.forename: Yuanyuan
authors.initials: Y
authors.lastname: Hou
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Haihe Education Park, 38 Tongyan Road, Tianjin 300353, People's Republic of China. Electronic address: minjiang@nankai.edu.cn.
authors.forename: Min
authors.initials: M
authors.lastname: Jiang
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Haihe Education Park, 38 Tongyan Road, Tianjin 300353, People's Republic of China. Electronic address: gangbai@nankai.edu.cn.
authors.forename: Gang
authors.initials: G
authors.lastname: Bai
mesh_terms: D000818:Animals; D002384:Catalysis / Q000187:drug effects*; D002460:Cell Line; D031180:Cirsium / Q000737:chemistry*; D057809:HEK293 Cells; D006490:Hemostatics / Q000494:pharmacology*; D006801:Humans; D008297:Male; D009638:Norepinephrine / Q000378:metabolism*; D010936:Plant Extracts / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D011941:Receptors, Adrenergic / Q000378:metabolism*; D014439:Tyramine / Q000031:analogs & derivatives / Q000494:pharmacology
chemical_list: D006490:Hemostatics; D010936:Plant Extracts; D011941:Receptors, Adrenergic; C036244:methyl-4-tyramine; D009638:Norepinephrine; D014439:Tyramine
keywords: Adrenergic receptor; Cirsium setosum; Norepinephrine; Tyramine