The development of new, safe, topical microbicides for intravaginal use for
the prevention of sexually transmitted diseases is imperative. Previous st
udies have suggested that bile salts may inhibit human immunodeficiency vir
us infection; however, their activities against other sexually transmitted
pathogens have not been reported. To further explore the potential role of
bile salts in preventing sexually transmitted diseases, we examined the in
vitro activities and cytotoxicities of select bile salts against Chlamydia
trachomatis, herpes simplex virus (types 1 and 2), Neisseria gonorrhoeae, a
nd human immunodeficiency virus in comparison to those of nonoxynol-9 and b
enzalkonium chloride using both primary cells and cell lines derived from t
he human female genital tract, We found that taurolithocholic acid 3-sulfat
e and a combination of glycocholic acid and taurolithocholic acid 3-sulfate
showed excellent activity against all of the pathogens assayed. Moreover,
taurolithocholic acid 3-sulfate alone or in combination was less cytotoxic
than nonoxynol-9 and benzalkonium chloride. Thus, taurolithocholic acid 3-s
ulfate alone or in combination warrants further evaluation as a candidate t
opical microbicidal agent.