title: Serine protease inhibitor 4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride (AEBSF) inhibits the rat embryo implantation in vivo and interferes with cell adhesion in vitro.
abstract: BACKGROUND
  This study was conducted to observe the in vivo effect of 4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride (AEBSF) on embryo implantation in rats and its in vitro effect on cell adhesion.
  
  
  METHODS
  The anti-implantation efficacy of AEBSF in rats was determined by counting the number of visible implanted embryos on day 8 of pregnancy following intrauterine (5 mg and 10 mg AEBSF per horn) or tail vein (10 mg AEBSF per rat) administration on day 3 of pregnancy. The effects of AEBSF on cell adhesion were detected, respectively, by using the mouse blastocysts-endometrial cells or the human umbilical vein endothelial cells (HUVECs)-HeLa cells co-culture model. The alteration in protein secretion pattern of HUVECs and HeLa cells was detected by the proteome analysis.
  
  
  RESULTS
  4-(2-Aminoethyl)benzenesulfonyl fluoride hydrochloride showed an in vivo inhibitory effect on embryo implantation in rat. In vitro, AEBSF could disturb the growth of blastocysts on endometrial cells and inhibit the adhesion of HeLa cells on HUVECs. The treatment of AEBSF could alter the protein secretion pattern of co-cultured HUVEC-HeLa cells.
  
  
  CONCLUSIONS
  4-(2-Aminoethyl)benzenesulfonyl fluoride hydrochloride might be a potential leading compound for novel contraceptives, and its inhibitory effect on implantation might result from the interference in extracellular matrix remodeling process.
authors.affiliation: NPFPC Key Laboratory of Contraceptives and Devices, Shanghai Institute of Planned Parenthood Research, Shanghai 200032, China.
authors.forename: Ya-hong
authors.initials: YH
authors.lastname: Jiang
authors.forename: Yan
authors.initials: Y
authors.lastname: Shi
authors.forename: Ya-ping
authors.initials: YP
authors.lastname: He
authors.forename: Jing
authors.initials: J
authors.lastname: Du
authors.forename: Run-sheng
authors.initials: RS
authors.lastname: Li
authors.forename: Hui-juan
authors.initials: HJ
authors.lastname: Shi
authors.forename: Zhao-gui
authors.initials: ZG
authors.lastname: Sun
authors.forename: Jian
authors.initials: J
authors.lastname: Wang
mesh_terms: D000282:Administration, Intravaginal; D000818:Animals; D001755:Blastocyst / Q000187:drug effects; D002448:Cell Adhesion / Q000187:drug effects; D002478:Cells, Cultured; D018920:Coculture Techniques; D003283:Contraceptives, Postcoital, Synthetic / Q000008:administration & dosage / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D010064:Embryo Implantation / Q000187:drug effects*; D004717:Endometrium / Q000166:cytology / Q000187:drug effects; D005260:Female; D006367:HeLa Cells; D061307:Human Umbilical Vein Endothelial Cells / Q000187:drug effects; D006801:Humans; D007275:Injections, Intravenous; D051379:Mice; D008813:Mice, Inbred ICR; D011247:Pregnancy; D011897:Random Allocation; D051381:Rats; D017207:Rats, Sprague-Dawley; D015842:Serine Proteinase Inhibitors / Q000008:administration & dosage / Q000494:pharmacology*; D013450:Sulfones / Q000008:administration & dosage / Q000494:pharmacology*
chemical_list: D003283:Contraceptives, Postcoital, Synthetic; D015842:Serine Proteinase Inhibitors; D013450:Sulfones; C002010:4-(2-aminoethyl)benzenesulfonylfluoride