Int Conf AIDS. 1996 Jul 7-12;11(2):16 (abstract no. We.A.510). Unique
Objective: To extend our studies on the range of activities of a
C31G-based microbicide to include isolates of Neisseria gonorrhoeae that
are sialylated on the terminal galactose moiety of the gonococcal
lipooligosaccharide and/or grown anaerobically, and thus mimic the in
vivo situation. Methods: C31G is a broad-spectrum agent effective
against gram positive and gram negative bacteria, fungi, and enveloped
viruses. It is composed of an equimolar mixture of an alkyl amine
N-oxide and an alkyl N-dimethylglycine (betaine), buffered with citric
acid. The chemical and physical properties of C31G can be altered by
changing the length of the alkyl chains. In the present study, alkyl
chain lengths of C12 vs C14/C16 were evaluated for efficacy against N.
gonorrhoeae strain F62. Bacteria were grown under either aerobic or
anaerobic conditions, and in the presence or absence of CMP-NANA to
generate sialylated and non-sialylated surface lipooligosaccahrides. The
efficacy of C31G was evaluated by determining the Minimum Inhibitory
Concentration (MIC). Results: The C14/C16 form of C31G consistently
showed increased efficacy as compared to the shorter alkyl chain C12
form (MIC's of 0.00032% vs .00125%). As expected, sialylated forms of N.
gonorrhoeae demonstrated resistance to human serum bacteriocidal
activity as compared with non-sialylated bacteria. On the other hand,
the effects of the microbicide C31G were not diminished either by growth
in anaerobic conditions, or by sialylation of the gonococci.
Conclusions: C31G is currently under evaluation for use as a vaginal
microbicide. Previous studies have shown efficacy against a variety of
STD pathogens including HIV, HSV, Treponema, Chlamydia, H. ducreyi and
C. albicans. In the present study, the compound has demonstrated potent
in vitro activity against N. gonorrhoeae under conditions expected in
vivo anaerobic and sialylation of surface lipooligosaccharides). 33505
and HD 3-3193.
*Betaine/CHEMISTRY *Neisseria gonorrhoeae/DRUG EFFECTS *Sexually
Transmitted Diseases/DRUG THERAPY