title: Synthesis, nanofeatures, in vitro thrombus lysis activity and in vivo thrombolytic activity of poly-alpha,beta-aspartyl-L-alanine.
abstract: OBJECTIVE
  Applying nanoscale assembly to the design of a thrombolytic agent.
  
  
  METHODS
  poly-alpha,beta-DL-aspartyl-L-alanine (molecular weight: 15726 atomic mass units) from the thermal polycondensation of DL-aspartic acid and the amidation of polysuccimide with L-alanine.
  
  
  METHODS
  The correlation of concentration and pH with nanofeatures, the correlation of concentration with in vitro thrombus lysis activity, the correlation of dose with the in vivo thrombolytic activity and the correlation of the dose with nanofeatures are all explained in this article.
  
  
  RESULTS
  Poly-alpha,beta-DL-aspartyl-L-alanine was concentration- (6.4 x 10(4,2,-4,-6,-8,-10,-12) nM) and pH-dependently (pH 1.2, 7.4 and 7.6) assembled to various nanospecies, exhibited concentration-dependent (4, 8 and 16 microM) lysis action in vitro and dose-dependent (5, 0.5 and 0.05 micromol/kg) thrombolytic action in vivo.
  
  
  CONCLUSIONS
  Upon entering the stomach, intestinal tract, blood and tissue fluids, poly-alpha,beta-DL-aspartyl-L-alanine assembled to small nanoparticles or nanoblocks to escape the entrapment by macrophages and exhibited desirable thrombolytic action.
authors.affiliation: College of Pharmaceutical Sciences, Capital Medical University, Beijing, 100069, PR China.
authors.forename: Lin
authors.initials: L
authors.lastname: Gui
authors.forename: Ming
authors.initials: M
authors.lastname: Zhao
authors.forename: Yinye
authors.initials: Y
authors.lastname: Wang
authors.forename: Yang
authors.initials: Y
authors.lastname: Qin
authors.forename: Jiangyuan
authors.initials: J
authors.lastname: Liu
authors.forename: Shiqi
authors.initials: S
authors.lastname: Peng
mesh_terms: D000818:Animals; D005343:Fibrinolytic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use*; D008297:Male; D008855:Microscopy, Electron, Scanning; D046529:Microscopy, Electron, Transmission; D049329:Nanostructures / Q000737:chemistry* / Q000648:ultrastructure; D011506:Proteins / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013927:Thrombosis / Q000188:drug therapy*
chemical_list: D005343:Fibrinolytic Agents; D011506:Proteins; C553661:poly-alpha,beta-aspartyl-alanine