Abstract

Although metronidazole is an effective anti-amoebic medication, it is mutagenic and some strains of Entamoeba histolytica resistant to this drug have begun to appear. The search for new anti-amoebic compounds is, therefore, justified. We have previously found that gossypol has a potent in-vitro anti-amoebic effect; we now show that this compound is also effective in-vivo. Hamsters with experimental amoebic hepatic abscess were fed acetic acid gossypol (0–45 mg kg−1) or metronidazole (30 or 45 mg kg−1) for 5 or 10 days. The experimental amoebic hepatic abscess size and the in-vitro cell density reached by trophozoite cultures from the experimental amoebic hepatic abscesses were scored. Gossypol and metronidazole reduced the experimental amoebic hepatic abscess. The smallest effect of gossypol was obtained with 5–45 mg kg−1 (23–31% score reduction) administered for 5 days whereas the most effective treatment corresponded to 30 mg kg−1 gossypol for 10 days (90% score reduction). Gossypol at 45 mg kg−1 for 10 days was toxic. The anti-amoebic effect of 30 mg kg−1, judged as the cell density score reduction compared with the control group, was comparable with that produced by 30 mg kg−1 metronidazole administered for 10 days. Although in molar concentration terms, gossypol was nine times more potent than metronidazole, the margin between the most effective and lethal doses of gossypol was relatively narrow. A combination of gossypol and metronidazole could be a more efficacious and less toxic anti-amoebic combination than the separate drugs.

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