A potential anti-implantation and spermicidal strategy: Putative derivatives of nonoxynol-9 and anti-inflammatory agents and their spermicidal activity

Objectives 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...

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Bibliographic Details
Published in:	The European journal of contraception & reproductive health care Vol. 11; no. 4; pp. 258 - 261
Main Authors:	Ingram, Matthew J., Zeller, Edel, Moss, Gary P., Hall, Charlotte E.
Format:	Journal Article
Language:	English
Published:	England Informa UK Ltd 01-12-2006 Taylor & Francis Taylor & Francis Ltd
Subjects:	Animals Anti-implantation Anti-Inflammatory Agents, Non-Steroidal - administration & dosage Anti-Inflammatory Agents, Non-Steroidal - pharmacology Apoptosis Birth control Boar spermatozoa Cell Survival - drug effects Contraceptive Derivatives Dose-Response Relationship, Drug Drug Therapy, Combination Ibuprofen Ibuprofen - administration & dosage Ibuprofen - pharmacology Indomethacin Indomethacin - administration & dosage Indomethacin - pharmacology Male Mass spectrometry Molecular weight Nonoxynol - administration & dosage Nonoxynol - pharmacology Nonoxynol-9 Sperm Motility - drug effects Spermatocidal Agents - administration & dosage Spermatocidal Agents - pharmacology Spermatozoa - drug effects Spermicide Swine
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Summary:	Objectives 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 µg 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.
ISSN:	1362-5187 1473-0782
DOI:	10.1080/13625180600907487