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Biological Activity and Metabolism of the Retinoid Axerophthene (Vitamin A Hydrocarbon)

National Cancer Institute, Bethesda, Maryland 20014 [D. L. N., C. A. F., A. B. R., J. M. S., M. B. S.], and BASF Aktiengesellschaft, 6700 Ludwigshafen am Rhein, Germany [A. N., J. P]

Biological properties of axerophthene, the hydrocarbon analog of retinol, have been studied both in vitro and in vivo. In tracheal organ culture axerophthene reversed keratinization caused by deficiency of retinoid in the culture medium; its potency was of the same order of magnitude as that of retinyl acetate. Axerophthene supported growth in hamsters fed vitamin A-deficient diets although less effectively than did retinyl acetate. Axerophthene was considerably less toxic than was retinyl acetate when administered repeatedly in high doses to rats. Administration of an equivalent p.o. dose of axerophthene caused much less deposition of retinyl palmitate in the liver than did the same dose of retinyl acetate, while a greater level of total retinoid was found in the mammary gland after administration of axerophthene.

Received 12/ 2/77. Accepted 3/ 8/78.