Sophorolipids, microbial glycolipids with anti-human immunodeficiency virus and sperm-immobilizing activities

Antimicrob Agents Chemother. 2005 Oct;49(10):4093-100. doi: 10.1128/AAC.49.10.4093-4100.2005.


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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / pharmacology*
  • Candida / chemistry
  • Cell Culture Techniques
  • Cell Line
  • Cell Survival / drug effects
  • Cytopathogenic Effect, Viral / drug effects
  • Dose-Response Relationship, Drug
  • Epithelial Cells / drug effects
  • Female
  • Glycolipids / chemical synthesis
  • Glycolipids / chemistry
  • Glycolipids / pharmacology*
  • Glycolipids / toxicity*
  • HIV-1 / drug effects
  • Humans
  • Interleukin-1 / analysis
  • Interleukin-1 / biosynthesis
  • Interleukin-8 / analysis
  • Interleukin-8 / biosynthesis
  • Male
  • Sperm Motility / drug effects*
  • Spermatocidal Agents / pharmacology*
  • Structure-Activity Relationship
  • Time Factors
  • Vagina / cytology


  • Anti-HIV Agents
  • Glycolipids
  • Interleukin-1
  • Interleukin-8
  • Spermatocidal Agents