Xue Y C, Wu S Y, Li Y, Zhang S H, Zhen Y S
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing.
Yao Xue Xue Bao. 1996;31(3):171-5.
Yungumycin, produced by a Streptomyces strain which was isolated from a soil sample collected in Guanping Nature Conservation Zone, Yunnan Province, China, has been verified to be identical with gougerotin. Determined by clonogenic assay, the IC50 of yungumycin to KB cells was found to be 1 microgram.ml-1. By spermatogonial assay, the activity of yungumycin was very close to that of 5-FU and MTX. Administered by i.p. route, yungumycin showed moderate inhibition against colon carcinoma 26 in mice. However, yungumycin by oral administration exerted highly inhibitory effects on both colon carcinoma 26 and sarcoma 180 (solid tumor) in mice and the inhibition rates reached 85% and 83%, respectively, at tolerable dose. Compared at equitoxic dose of 1/6 LD50, the inhibitory effect of yungumycin (15 mg.kg-1) on sarcoma 180 was similar to that of 5-FU (40 mg.kg-1), showing 72% and 70% tumor inhibition, respectively. Initially, gougerotin was reported as an antibacterial antibiotic without mentioning its antitumor activity. The present studies demonstrate that yungumycin (gougerotin), by oral administration, may be useful in cancer chemotherapy.
云谷霉素由从中国云南省关坪自然保护区采集的土壤样本中分离出的一株链霉菌产生，经证实与谷氏菌素相同。通过克隆形成试验测定，云谷霉素对KB细胞的IC50为1微克/毫升。通过精原细胞试验，云谷霉素的活性与5-氟尿嘧啶和甲氨蝶呤非常接近。经腹腔注射给药，云谷霉素对小鼠结肠癌26显示出中度抑制作用。然而，口服云谷霉素对小鼠结肠癌26和肉瘤180（实体瘤）均具有高度抑制作用，在可耐受剂量下抑制率分别达到85%和83%。在1/6 LD50的等毒性剂量下比较，云谷霉素（15毫克/千克）对肉瘤180的抑制作用与5-氟尿嘧啶（40毫克/千克）相似，肿瘤抑制率分别为72%和70%。最初，谷氏菌素被报道为一种抗菌抗生素，未提及其抗肿瘤活性。目前的研究表明，口服云谷霉素（谷氏菌素）可能对癌症化疗有用。
