title: A potential anti-implantation and spermicidal strategy: putative derivatives of nonoxynol-9 and anti-inflammatory agents and their spermicidal activity.
abstract: OBJECTIVE
  We report the synthesis of novel ester derivatives of nonoxynol-9, an approved spermicidal agent, using the non-steroidal inflammatory drugs (NSAIDs) ibuprofen and indomethacin. Indomethacin has previously been shown to inhibit the implantation of the fertilised ovum into the uterus wall of pregnant rats. It is proposed that nonoxynol-9, in combination with a non-selective NSAID may exhibit both anti-implantation and spermicidal properties.
  
  
  METHODS
  Both novel derivatives and nonoxynol-9 were then tested on boar spermatozoa in order to establish if spermicidal activity was retained following the esterification.
  
  
  RESULTS
  The results showed that both the ibuprofen and indomethacin derivatives enabled complete cell death of boar spermatozoa at a concentration of 100 microg ml(-1), which is comparable to nonoxynol-9 at the same concentration.
  
  
  CONCLUSIONS
  These results indicate that NSAID derivatives of nonoxynol-9 retain the activity of the parent molecule and may have other advantages associated with the molecular incorporation of the NSAID moieties and their anti-implantation activity.
authors.affiliation: School of Pharmacy and Biomolecular Sciences, University of Brighton, Cockcroft Building, Moulsecoomb, Brighton BN2 4GJ, UK. mji@bton.ac.uk
authors.forename: Matthew J
authors.initials: MJ
authors.lastname: Ingram
authors.forename: Edel
authors.initials: E
authors.lastname: Zeller
authors.forename: Gary P
authors.initials: GP
authors.lastname: Moss
authors.forename: Charlotte E
authors.initials: CE
authors.lastname: Hall
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004359:Drug Therapy, Combination; D007052:Ibuprofen / Q000008:administration & dosage / Q000494:pharmacology; D007213:Indomethacin / Q000008:administration & dosage / Q000494:pharmacology; D008297:Male; D017137:Nonoxynol / Q000008:administration & dosage / Q000494:pharmacology*; D013081:Sperm Motility / Q000187:drug effects; D013089:Spermatocidal Agents / Q000008:administration & dosage / Q000494:pharmacology*; D013094:Spermatozoa / Q000187:drug effects*; D013552:Swine
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D013089:Spermatocidal Agents; D017137:Nonoxynol; D007052:Ibuprofen; D007213:Indomethacin