Studies on terreic acid.

Abstract

It was found that Aspergillus sp. No. Y-8980 which was isolated from a soil sample collected at Yoron Island in Kagoshima Prefecture belonged to Aspergillus terreus group by morphological observation. The active substance produced by the strain was obtained with a high yield in sucrose-yeast extract medium and extracted by chloroform, ethyl acetate and n-butanol at pH 2.4 approximately 2.6 from the culture broth. The substance was crystallized from chloroform and ethyl acetate after charcoal treatment of the crude crystal. From various physico-chemical properties, it was found that the substance was identical to terreic acid. Terreic acid showed MICs of 25 approximately 100 mcg/ml, 12.5 mcg/ml and 50 mcg/ml against Gram-positive and Gram-negative bacteria, Xanthomonas oryzae and Xanthomonas citri, respectively, but it did not control Pseudomonas, fungi and yeast. The LD50 was 75 mg/kg i.p. and i.v. in mice. With regards to the anti-tumor effect, the morphological degeneration on HeLa cells (human carcinoma cells) was observed in the concentrations of more than 6.25 mcg/ml of terreic acid. An increase of body weight of mice caused by Ehrlich ascites carcinoma cells was not definitely observed by the daily administration of 150 mcg of terreic acid per mouse for 8 consecutive days. Above showed the enough survival effect in dd mice implanted with Ehrlich ascites carcinoma cells, and the effect also was demonstrated by anatomies of mice.