title: Evaluation of the spermicidal and contraceptive activity of Platycodin D, a Saponin from Platycodon grandiflorum.
abstract: BACKGROUND
  The extract of Platycodon grandiflorum has been reported to have effective spermicidal activity. This study was designed to evaluate the spermicidal and contraceptive activity, as well as the safety, of Platycodin D (PD), a major saponin in Platycodon grandiflorum.
  
  
  METHODS
  Using the computer-aided sperm analysis (CASA) test criteria, the sperm-immobilizing activity of PD was studied using highly motile human sperm. The sperm viability was assessed by fluorescent staining using SYBR-14 (living sperm) and propidium iodide (dead sperm). The sperm membrane integrity was assessed by evaluating the hypo-osmotic swelling (HOS) and examinations by transmission electron microscopy (TEM) and scanning electron microscopy (SEM). The in vivo contraceptive efficacy was evaluated in rats using post-intrauterine PD application. The comet assay was employed to determine whether PD caused DNA damage in the sperm. Vaginal biopsies were also performed to determine whether the PD gel induced vaginal inflammation.
  
  
  RESULTS
  A dose-dependent effect of PD on the sperm motility and viability was observed. The maximum spermicidal effect was observed with a 0.25 mM concentration of PD. More than 70% of the PD-treated sperm lost their HOS responsiveness at a concentration of 0.20 mM PD, indicating that PD caused injury to the sperm plasma membrane. TEM and SEM revealed significant damage to both the head and tail membranes of the sperm. PD decreased the fertility to zero in rats, was non-DNA damaging and was not harmful to the vaginal tissue in the rats.
  
  
  CONCLUSIONS
  PD has significant spermicidal activity that should be explored in further studies.
authors.affiliation: Department of Nutrition, Daping Hospital and Research Institute of Surgery, Third Military Medical University, Chongqing, PR China ; Research Center for Nutrition and Food Safety, Third Military Medical University, Chongqing, PR China.
authors.forename: Zongliang
authors.initials: Z
authors.lastname: Lu
authors.forename: Leiguang
authors.initials: L
authors.lastname: Wang
authors.forename: Rui
authors.initials: R
authors.lastname: Zhou
authors.forename: Yi
authors.initials: Y
authors.lastname: Qiu
authors.forename: Liuna
authors.initials: L
authors.lastname: Yang
authors.forename: Chanyu
authors.initials: C
authors.lastname: Zhang
authors.forename: Min
authors.initials: M
authors.lastname: Cai
authors.forename: Mantian
authors.initials: M
authors.lastname: Mi
authors.forename: Hongxia
authors.initials: H
authors.lastname: Xu
mesh_terms: D000328:Adult; D000818:Animals; D002470:Cell Survival / Q000187:drug effects; D020552:Comet Assay; D003267:Contraception; D005260:Female; D006801:Humans; D008297:Male; D009092:Mucous Membrane / Q000187:drug effects; D031238:Platycodon / Q000737:chemistry*; D051381:Rats; D012503:Saponins / Q000494:pharmacology* / Q000633:toxicity; D013081:Sperm Motility / Q000187:drug effects; D013089:Spermatocidal Agents / Q000494:pharmacology* / Q000633:toxicity; D013094:Spermatozoa / Q000166:cytology / Q000648:ultrastructure; D014315:Triterpenes / Q000494:pharmacology* / Q000633:toxicity; D014621:Vagina / Q000187:drug effects; D055815:Young Adult
chemical_list: D012503:Saponins; D013089:Spermatocidal Agents; D014315:Triterpenes; C108953:platycodin D