Yamamoto H, Moriyama K, Jinnouchi H, Yagishita K
Jpn J Antibiot. 1980 Mar;33(3):320-8.
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.
从鹿儿岛县与论岛采集的土壤样本中分离出的曲霉属菌株Y - 8980，经形态学观察属于土曲霉群。该菌株产生的活性物质在蔗糖酵母提取物培养基中高产获得，并在pH约为2.4至2.6时用氯仿、乙酸乙酯和正丁醇从培养液中萃取。粗晶体经活性炭处理后，该物质从氯仿和乙酸乙酯中结晶出来。从各种理化性质来看，发现该物质与地霉酸相同。地霉酸对革兰氏阳性菌和革兰氏阴性菌、稻黄单胞菌和柑橘黄单胞菌的最低抑菌浓度分别约为25至100 mcg/ml、12.5 mcg/ml和50 mcg/ml，但对假单胞菌、真菌和酵母无效。小鼠腹腔注射和静脉注射的半数致死量为75 mg/kg。关于抗肿瘤作用，在土霉酸浓度超过6.25 mcg/ml时观察到HeLa细胞（人癌细胞）的形态退化。连续8天每天给每只小鼠腹腔注射150 mcg土霉酸，未明确观察到艾氏腹水癌细胞导致的小鼠体重增加。上述结果表明，对接种艾氏腹水癌的dd小鼠有足够的生存效果，解剖小鼠也证实了这一效果。
