Antituberculous Activity and Toxicity of Lupulon for the Mouse.

Abstract
Lupulon, a fat-soluble antibiotic derived from hops, has relatively low in vitro activity (1:40,000) as compared with other antituberculous agents, but is active when given orally or intramusc. against exptl. mouse infections of Mycobacterium tuberculosis. Following intramusc. admn., significantly lower nos. of acid-fast organisms occur in lesions of treated animals. The approx. nos. relative to the control were: In the liver, 34/1; heart, 8/1, spleen, 4/1; and lungs, 4/1; but without difference in the kidneys. In orally treated animals the ratios were; Liver, 10/1; heart, 3/1; spleen 10/1; lungs, 5/1; and kidneys, 2/1. The over-all difference was a reduction of approx. 4/1 by either route of admn. Lupulon given intramusc. within its effective range produced some foci of degeneration in renal tubules. Such pathologic changes were not observed in infected animals given this antibiotic orally in effective doses. The single LD50 on intramusc. admn. was 600 mg./kg. in mice; on oral application, 1500 mg./kg.
Keywords