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Lapachol [2-hydroxy-3(3-methyl-2-butenyl)-1,4-naphthoquinone] suspended in mineral oil and Freund's incomplete adjuvant administered by gavage to mice significantly reduced Schistosoma mansoni cercarial penetration and worm burdens between 8% and 100%, depending on dosage. High toxicity resulted from this treatment. Lapachol (0.9%) in the diet of mice reduced infection by 80% after 24 hours of feeding and by 96.9% after 3 days of feeding. Protection declined from 70% to 35% from 0 to 3 days after a single 24-hour feeding period. The sodium salt of lapachol at 0.5% in the drinking water reduced infection between 26.7% and 72.6%. Mice were protected from tail immersion and whole-body-wading challenge infections. Ultraviolet spectrophotometry demonstrated that the lapachol is secreted, presumably by the sebaceous glands, onto the skin where it acts as a topical barrier to penetration. Toxicity with dietary treatment (2,600 mg lapachol/kg mouse body wt./day) was limited to body-weight loss, which was completely recovered 7 days after treatment. No blood or histopathological changes were seen in mice treated for 4 days.
Accepted for publication October 13, 1973.
The opinions or assertions contained herein are the private ones of the author and are not to be construed as official or reflecting the views of the Navy Department or the naval service at large.
The experiments reported herein were conducted according to the principles outlined in the Animal Welfare Act (PL 89-544 as amended) and followed the guidelines prescribed in DHEW Publication No. (NIH) 7223, formerly PHS Publication No. 1024, "Guide for Laboratory Animal Facilities and Care."
* From the Bureau of Medicine and Surgery, Navy Department, Research Task No. MF12.524.009.1004BC61.
Present address: New York State Veterinary College, Cornell University, Ithaca, New York 14850.
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