Xue Y C, Chen W J, Dai J, Qi C Q, Zhen Y S
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050.
Yao Xue Xue Bao. 1997 Sep;32(9):647-51.
Antibiotic G0069A, produced by a Streptomyces strain isolated from a soil sample collected in Yunnan Province, China, has been verified as a clavam peptide. Determined by MTT assay, G0069A showed highly potent cytotoxicity to cancer cells with multidrug resistance. The IC50 values of G0069A to KB and KB/VCR cells were 0.60 and 0.46 mumol.L-1, and to MCF-7 and MCF-7/ADM cells were 1.4 and 1.2 mumol.L-1, respectively. G0069A displayed equally potent cytotoxicity to the parent cell lines and their resistant sublines. When administered by i.v. or i.p. route at tolerable doses, G0069A exhibited markedly inhibitory effect on the growth of sarcoma 180 and hepatoma 22 in mice. At dose level of 3 mg.kg-1, i.v., x3, sarcoma 180 and hepatoma 22 were suppressed by 87%(P < 0.01) and 72%(P < 0.01), respectively. The results indicate that G0069A is a beta-lactam antibiotic showing antitumor activity.
从中国云南省采集的土壤样本中分离出的一株链霉菌产生的抗生素G0069A已被确认为一种棒酸肽。通过MTT法测定，G0069A对具有多药耐药性的癌细胞显示出高效的细胞毒性。G0069A对KB和KB/VCR细胞的IC50值分别为0.60和0.46μmol·L-1，对MCF-7和MCF-7/ADM细胞的IC50值分别为1.4和1.2μmol·L-1。G0069A对亲本细胞系及其耐药亚系表现出同等强效的细胞毒性。当以可耐受剂量通过静脉注射或腹腔注射途径给药时，G0069A对小鼠肉瘤180和肝癌22的生长表现出明显的抑制作用。在静脉注射剂量为3mg·kg-1，连续给药3次时，肉瘤180和肝癌22分别被抑制87%（P<0.01）和72%（P<0.01）。结果表明，G0069A是一种具有抗肿瘤活性的β-内酰胺抗生素。
