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Hum. Reprod. Advance Access originally published online on November 17, 2006
Human Reproduction 2007 22(3):708-716; doi:10.1093/humrep/del448
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© The Author 2006. Published by Oxford University Press on behalf of the European Society of Human Reproduction and Embryology. All rights reserved. For Permissions, please email: journals.permissions@oxfordjournals.org

Novel disulphide esters of carbothioic acid as potent, non-detergent spermicides with low toxicity to Lactobacillus and HeLa cells in vitro

R.K. Jain1, J.P. Maikhuri1, S.T.V.S. Kiran Kumar2, V.L. Sharma2, A.K. Dwivedi3, K. Mitra4, V.K. Bajpai4 and G. Gupta1,5

1 Division of Endocrinology 2 Division of Medicinal Chemistry 3 Division of Pharmaceutics and 4 Electron Microscopy Unit, Central Drug Research Institute, Lucknow, Uttar Pradesh, India

5 To whom correspondence should be addressed at: Division of Endocrinology, Central Drug Research Institute, Chhattar Manzil, PO Box 173, Lucknow 226001, Uttar Pradesh, India. E-mail: gupta.gopal{at}rediffmail.com

BACKGROUND: The design, synthesis, characterization and evaluation of a novel series of non-detergent spermicides has led to the discovery of two unique molecules (DSE-36 and DSE-37) that were ~25 times more potent spermicides than nonoxynol-9 (N-9). METHODS: Normal human spermatozoa were used to assess the spermicidal activity (Sander–Cramer Assay), the effect on sperm-membrane integrity [hypo-osmotic swelling test (HOST)], supravital staining and scanning electron microscopy (SEM) and the induction of apoptosis [fluorescein isothiocyanate (FITC) Annexin-V and JC-1 labelling using flow cytometry] by the new class of compounds. HeLa and Lactobacillus cultures were used to assess the cytotoxicity of compounds and their compatibility to normal vaginal flora, respectively. RESULTS: Compounds DSE-36 and DSE-37 exhibited a strong spermicidal activity [minimum effective concentration (MEC) = 0.002%], which was ~25 times more potent than that of N-9 and Sapindus saponins (MEC = 0.05%). As compared with surfactants, DSE-36 and DSE-37 were found to be safer at MEC towards the growth and survival of Lactobacilli and HeLa cells in vitro and to have a milder effect on sperm plasma membrane. At EC50 both induced apoptosis in sperm cells as characterized by increased labelling with Annexin-V and decreased polarization of sperm mitochondria. CONCLUSION: Preliminary studies have revealed that in sharp contrast to the non-specific surfactant action of N-9, DSE-36 and DSE-37 have a highly potent, mechanism-based, detrimental action on human sperm. The unique ability of these non-detergent molecules to selectively kill sperm and spare Lactobacilli and HeLa cells at MEC values much lower than that required for N-9 indicates their potential as superior ingredients for formulation into microbicidal contraceptives.

Key words: contraception/non-detergent spermicides/spermicidal activity/selective toxicity

Submitted on August 2, 2006; resubmitted on October 10, 2006; accepted on October 19, 2006.


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R. K. Jain, A. Jain, J. P. Maikhuri, V. L. Sharma, A. K. Dwivedi, S.T.V.S. Kiran Kumar, K. Mitra, V. K. Bajpai, and G. Gupta
In vitro testing of rationally designed spermicides for selectively targeting human sperm in vagina to ensure safe contraception
Hum. Reprod., March 1, 2009; 24(3): 590 - 601.
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