Evaluation of poly(styrene-4-sulfonate) as a preventive agent for conception and sexually transmitted diseases.
A commercial preparation of a sodium polystyrene sulfonate (designated as N-PSS; its molecular weight is 500000 daltons) was tested as an inhibitor of sperm function and as a preventive agent for conception and the transmission of sexually transmitted diseases. The polymer is an irreversible inhibitor of hyaluronidase and acrosin; its IC50 values are 5.7 microg/mL and 0.5 microg/mL, for hyaluronidase and acrosin, respectively. N-PSS is also a stimulus of human sperm acrosomal loss. It produces maximal acrosomal loss at 2.5 microg/mL. Contraception in rabbits is nearly complete when rabbit spermatozoa are pretreated with 0.5 mg/mL of N-PSS before artificial insemination; however, N-PSS does not immobilize spermatozoa at concentrations as high as 50 mg/mL. N-PSS has broad spectrum antiviral and antibacterial activities. Infection by human immunodeficiency virus and herpes simplex virus are inhibited by N-PSS; 3-log reductions are produced by 7 microg/mL and 3 microg/mL, respectively. N-PSS is active against Chlamydia trachomatis and Neisseria gonorrhoeae. At 1 mg/mL, N-PSS inhibits chlamydial infectivity by more than 90%. N-PSS produces a 3-log reduction in gonococcal growth at 15 microg/mL. In contrast, N-PSS (5 mg/mL) does not affect the growth of Lactobacillus (normal component of the vaginal flora). N-PSS can be classified as a noncytotoxic contraceptive antimicrobial agent. These properties justify bringing a polystyrene sulfonate into clinical trials for its evaluation as a preventive agent for conception and several sexually transmitted diseases.
Anderson
R A
RA
TOPCAD Program and the Department of Obstetrics and Gynecology, Rush Medical Center, Chicago, Illinois 60612, USA. randerso@rpslmc.edu
Feathergill
K
K
Diao
X
X
Cooper
M
M
Kirkpatrick
R
R
Spear
P
P
Waller
D P
DP
Chany
C
C
Doncel
G F
GF
Herold
B
B
Zaneveld
L J
LJ
D000818:Animals; D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents / Q000494:pharmacology*; D000998:Antiviral Agents / Q000494:pharmacology; D002692:Chlamydia trachomatis / Q000187:drug effects; D005260:Female; D006678:HIV / Q000187:drug effects; D006801:Humans; D006821:Hyaluronoglucosaminidase / Q000037:antagonists & inhibitors*; D007315:Insemination, Artificial; D008297:Male; D008826:Microbial Sensitivity Tests; D009344:Neisseria gonorrhoeae / Q000187:drug effects; D011137:Polystyrenes / Q000494:pharmacology*; D011817:Rabbits; D012749:Sexually Transmitted Diseases / Q000517:prevention & control* / Q000635:transmission; D018139:Simplexvirus / Q000187:drug effects; D013089:Spermatocidal Agents / Q000494:pharmacology*; D013094:Spermatozoa / Q000187:drug effects* / Q000502:physiology
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D000998:Antiviral Agents; D011137:Polystyrenes; D013089:Spermatocidal Agents; C003321:polystyrene sulfonic acid; D006821:Hyaluronoglucosaminidase