Arch Virol (1997) 142: 2225±2235
The effect of gramicidin, a topical contraceptive
and antimicrobial agent with anti-HIV activity,
against herpes simplex viruses type 1 and 2 in vitro
A. S. Bourinbaiar and C. F. Coleman
Metatron, Inc., New York, New York, U.S.A.
Accepted June 26, 1997
Summary. The effect of an anti-HIV compound, gramicidin, previously used as
a topical antibiotic and vaginal contraceptive, on the replication of herpes
simplex viruses (HSV) type 1 and 2 has been examined. Human WI-38
®broblasts were inoculated with either HSV type in the presence of serial
dilutions of gramicidin and reduction in viral yield was measured by ELISA.
The 50% inhibitory dose (IC
) of gramicidin against 3 HSV-1 and 4 HSV-2
isolates was equal to 0.3 mg/ml and was comparable to the ef®cacy of the anti-
HSV agent acyclovir (ACV). The IC
of gramicidin required to protect WI-38
from cytolytic effect of HSV was 10 mg/ml at day 5 postinfection, indicating
that at this time point the activity of gramicidin was inferior than that of ACV.
Nevertheless, gramicidin suppressed the replication of ACV-resistant thymidine
kinase and DNA polymerase HSV mutants at doses effective against ACV-
sensitive strains. The results suggest that the antimicrobial and spermostatic
agent, gramicidin, has potential against sexually transmitted diseases (STDs)
and for prophylaxis of sex-borne HIV and HSV infections.
Symptomatic human herpes simplex virus type 1 (HSV-1) infections are fairly
benign in immunocompetent individuals as HSV-caused oropharyngeal sores
tend to disappear spontaneously. Primary clinical manifestations of HSV-2
infection, which is mainly transmitted sexually, are anogenital lesions [12, 24].
Genital herpes affects one third of the world's population, and among people
with human immunode®ciency virus (HIV) the incidence may be as high as 80
percent . HSV infections are particularly severe and even life-threatening to
patients with acquired immune de®ciency syndrome . Only 20 percent of
herpes seropositive persons have symptomatic infection. The rest of them are
asymptomatic but nevertheless are able to shed the virus. In view of the high
prevalence of genital herpes and its cofactor role in enhancing sex-borne HIV
transmission the herpesviruses are of particular concern [7, 14].