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Antimicrobial Agents and Chemotherapy, October 2005, p. 4093-4100, Vol. 49, No. 10
0066-4804/05/$08.00+0     doi:10.1128/AAC.49.10.4093-4100.2005
Copyright © 2005, American Society for Microbiology. All Rights Reserved.

Sophorolipids, Microbial Glycolipids with Anti-Human Immunodeficiency Virus and Sperm-Immobilizing Activities

Vishal Shah,1 Gustavo F. Doncel,2 Theodoros Seyoum,2 Kristin M. Eaton,2 Irina Zalenskaya,2 Rena Hagver,1 Abul Azim,1 and Richard Gross1*

NSF Center for Biocatalysis and Bioprocessing of Macromolecules, Polytechnic University, Six Metrotech Center, Brooklyn, New York 11201,1 CONRAD, Department of Obstetrics and Gynecology, Eastern Virginia Medical School, Norfolk, Virginia, 235072

Received 9 March 2005/ Returned for modification 22 May 2005/ Accepted 1 August 2005

The increased incidence of human immunodeficiency virus (HIV)/AIDS disease in women aged 15 to 49 years has identified the urgent need for a female-controlled, efficacious, and safe vaginal topical microbicide. To meet this challenge, sophorolipid (SL) produced by Candida bombicola and its structural analogs have been studied in this report for their spermicidal, anti-HIV, and cytotoxic activities. The sophorolipid diacetate ethyl ester derivative is the most potent spermicidal and virucidal agent of the series of SLs studied. Its virucidal activity against HIV and sperm-immobilizing activity against human semen are similar to those of nonoxynol-9. However, it also induced enough vaginal cell toxicity to raise concerns about its applicability for long-term microbicidal contraception. Its structure-activity relationship has been established for creating new analogs with less cytotoxicity and higher activity.


* Corresponding author. Mailing address: NSF Center for Biocatalysis and Bioprocessing of Macromolecules, Polytechnic University, Six Metrotech Center, Brooklyn, NY 11201. Phone: (718) 260-3024. Fax: (718) 260-3075. E-mail: rgross{at}poly.edu.


Antimicrobial Agents and Chemotherapy, October 2005, p. 4093-4100, Vol. 49, No. 10
0066-4804/05/$08.00+0     doi:10.1128/AAC.49.10.4093-4100.2005
Copyright © 2005, American Society for Microbiology. All Rights Reserved.




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