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Amoebicidal Activity of Bismuthoxy p-N-Glycolyl-Arsanilate and 7-Iodo-4-(1-Methyl-4-Diethylamino-Butylamino)Quinoline Diphosphate

1. Bismuthoxy p-N-glycolylarsanilate (Win 1011; "WIA") is amoebacidal in vitro at a dilution of 1:30,000 to 1:35,000 when tested against Endamoeba histolytica in Hansen's egg infusion medium.

2. 7-Iodo-4-(1-methyl-4-diethylaminobutylamino)quinoline diphosphate (Win 246; SN-7620-5) is amoebacidal in vitro at a dilution range of 1:3,000 to 1:7,500; it is slightly more active than chloroquine diphosphate (Win 244; SN-7618-5). Both compounds are more active than chiniofon or diiodo-oxyquinoline under similar conditions.

3. Examination of the cecum showed that all hamsters (C. auratus) of our colony weighing more than 75 grams were naturally infected with Endamoeba criceti, and it was demonstrated that a five day course of oral medication with carbarsone, chiniofon or diiodo-oxyquinoline resulted in elimination of this infestation. It was concluded that the natural infection of the hamster with E. criceti is suitable for testing the amoebacidal activity of compounds which might be expected to reach the large intestine in sufficient concentration to be effective in the treatment of intestinal amoebiasis.

4. Win 246, the iodine analog of chloroquine, is effective in freeing hamsters of their intestinal amoebae when administered at toxic levels; chloroquine is ineffective in hamsters at dose levels which are lethal in five days.

5. Win 1011 is highly effective in clearing hamsters of E. criceti. The activity of this drug on a weight basis is greater than that of chiniofon or diiodo-oxyquin-oline and is slightly less than the activity of carbarsone. Win 1011 did not produce any evidence of toxicity when administered to hamsters for five days at ten times the dose level required to clear all test animals; carbarsone caused deaths when the dose level was three times greater than that required to clear all test animals.

6. Win 1011 appeared to be completely nontoxic when given orally to humans in therapeutic doses of 0.5 gm three times daily for ten days. In view of the low toxicity and preliminary reports of therapeutic efficacy in the treatment of intestinal amoebiasis it is recommended that Win 1011 be given a more extensive clinical trial and careful evaluation.

¹ Sterling-Winthrop Research Institute, Rensselaer, N. Y.