title: Spermicidal and contraceptive potential of desgalactotigonin: a prospective alternative of nonoxynol-9.
abstract: Crude decoction of Chenopodium album seed showed spermicidal effect at MIC 2 mg/ml in earlier studies. Systematic isolation, characterization and evaluation revealed that the major metabolite Desgalactotigonin (DGT) is the most effective principle in both in vitro and in vivo studies. The in vitro studies comprises (a) rat and human sperm motility and immobilizing activity by Sander-Cramer assay; (b) sperm membrane integrity was observed by HOS test and electron microscopy; (c) microbial potential was examined in Lactobacillus broth culture, and (d) the hemolytic index was determined by using rat RBCs. The in vivo contraceptive efficacy was evaluated by intra uterine application of DGT in rat. Lipid peroxidation and induction of apoptosis by DGT on human spermatozoa were also studied. The minimum effective concentration (MEC) of DGT that induced instantaneous immobilization in vitro was 24.18 µM for rat and 58.03 µM for human spermatozoa. Microbial study indicated DGT to be friendly to Lactobacillus acidophilus. Implantation was prevented in DGT treated uterine horn while no hindrance occurred in the untreated contra lateral side. At the level of EC50, DGT induced apoptosis in human spermatozoa as determined by increased labeling with Annexin-V and decreased polarization of sperm mitochondria. Desgalactotigonin emerged 80 and 2×10(4) times more potent than the decoction and Nonoxynol-9 respectively. It possesses mechanism based detrimental action on both human and rat spermatozoa and spares lactobacilli and HeLa cells at MEC which proves its potential as a superior ingredient for the formulation of a contraceptive safer/compatible to vaginal microflora.
authors.affiliation: Department of Chemistry, Indian Institute of Chemical Biology, Council of Scientific and Industrial Research, Jadavpur, Kolkata, West Bengal, India.
authors.forename: Debanjana
authors.initials: D
authors.lastname: Chakraborty
authors.affiliation: Department of Chemistry, Indian Institute of Chemical Biology, Council of Scientific and Industrial Research, Jadavpur, Kolkata, West Bengal, India.
authors.forename: Arindam
authors.initials: A
authors.lastname: Maity
authors.affiliation: Department of Pharmaceutical Technology, Division of Medicinal and Pharmaceutical Chemistry, Jadavpur University, Kolkata, West Bengal, India.
authors.forename: Tarun
authors.initials: T
authors.lastname: Jha
authors.affiliation: Department of Chemistry, Indian Institute of Chemical Biology, Council of Scientific and Industrial Research, Jadavpur, Kolkata, West Bengal, India.
authors.forename: Nirup Bikash
authors.initials: NB
authors.lastname: Mondal
mesh_terms: D000818:Animals; D017209:Apoptosis / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D027463:Chenopodium album; D003270:Contraceptive Agents / Q000494:pharmacology*; D006801:Humans; D015227:Lipid Peroxidation / Q000187:drug effects; D008297:Male; D017137:Nonoxynol / Q000494:pharmacology; D010936:Plant Extracts / Q000494:pharmacology*; D051381:Rats; D012503:Saponins / Q000494:pharmacology*; D013081:Sperm Motility / Q000187:drug effects*; D013089:Spermatocidal Agents / Q000494:pharmacology*; D013094:Spermatozoa / Q000187:drug effects*; D013256:Steroids / Q000494:pharmacology*
chemical_list: D003270:Contraceptive Agents; D010936:Plant Extracts; D012503:Saponins; D013089:Spermatocidal Agents; D013256:Steroids; C513758:degalactotigonin; D017137:Nonoxynol