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Microbicidal activity of C31G against N. gonorrhoeae under conditions that mimic the in vivo situation.
Malamud D; Douglas A; Rest R; Biosyn, Phila., PA. Fax: 215-387-5332.
January 30, 1997
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