Ph. Katelaris et al., ACTIVITY OF METRONIDAZOLE, AZITHROMYCIN AND 3 BENZIMIDAZOLES ON GIARDIA-LAMBLIA GROWTH AND ATTACHMENT TO A HUMAN INTESTINAL-CELL LINE, Alimentary pharmacology & therapeutics, 8(2), 1994, pp. 187-192
Background: Attachment of Giardia lamblia trophozoites to enterocytes
is essential for colonization of the small intestine and is considered
a prerequisite for Giardia-induced enterocyte damage. Inhibition of a
ttachment may therefore have therapeutic potential. Methods: Enterocyt
e-like differentiated Caco-2 cells were used as a biologically appropr
iate attachment surface to determine the effect of three benzimidazole
compounds (albendazole, mebendazole and thiabendazole), azithromycin
and metronidazole on Giardia attachment. The results were compared wit
h the ability for each drug to inhibit Giardia growth, measured using
[H-3]-thymidine uptake. Results: The benzimidazoles inhibited Giardia
attachment at much lower concentrations than did metronidazole. Howeve
r, metronidazole was a much more potent inhibitor of growth than any o
f the benzimidazoles. Azithromycin did not significantly impair Giardi
a attachment or growth. The benzimidazoles decrease attachment but are
less giardiacidal than metronidazole. Conclusion: This model appears
useful for testing potential antigiardial compounds and investigating
mechanisms of drug action.