Evaluation of the Spermicidal and Contraceptive Activity of Platycodin D, a Saponin from Platycodon grandiflorum

Abstract

BackgroundThe 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.MethodsUsing 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.ResultsA 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.ConclusionPD has significant spermicidal activity that should be explored in further studies.

The importance of transmission electron microscopy analysis of spermatozoa: Diagnostic applications and basic research

“…The damage that PVP causes to the sperm membranes can easily be observed by TEM analysis. TEM examination has been carried out to evaluate in vitro the spermicidal activity of different natural compounds [Saha et al 2010;Lu et al 2013] and non-detergent spermicidal compounds [Jain et al 2010]. The TEM method enables the detection of the harmful effect of these substances on the sperm membrane.…”

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“…For this reason, determination of DNA damage is important with regard to determination of infertility (Hamada et al, ). The single cell gel electrophoresis, also known as comet assay, is a method that can directly measure DNA damage, and is especially precise when determining DNA errors associated with double‐strand breaks (Trivedi et al, ; Lu et al, ; Ahmed, ; Namoju et al, ). According to our comet assay results, the 20 mg/kg CTL‐administered group had significantly increased tail movement percentage, an indicator of DNA damage induced by CTL.…”

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“…Luan et al (2014) (Takagi and Lee, 1972) In humans, there is a potential for some negative effects of excessive intake of saponins, including local effects on gut mucosa and secondary effects produced by mineral interactions decreasing availability for absorption (Milgate and Roberts, 1995). A dose-dependent effect of PD on the sperm motility and viability was reported (Lu et al, 2013). The maximum spermicidal effect was observed with a 0.25 mM concentration of PD.…”