甄永苏, 李电东, 林赴田, 李茜, 田佩玉, 薛玉川, 杨小平. 争光霉素A5和争光霉素A2的抗肿瘤作用与毒性研究J. 药学学报, 1979, 14(2): 83-90.
引用本文: 甄永苏, 李电东, 林赴田, 李茜, 田佩玉, 薛玉川, 杨小平. 争光霉素A5和争光霉素A2的抗肿瘤作用与毒性研究J. 药学学报, 1979, 14(2): 83-90.
Zhen Yongsu, Li Di,ong, Lin Futian, Li Qian, Tian Peiyu, Xue Yuchuan, , Yang xiaoping. STUDY ON THE ANTITUMOR ACTIVITIES AND THE TOXICITIES OF ZHENGGUANGMYCINS A5 AND A2J. Acta Pharmaceutica Sinica, 1979, 14(2): 83-90.
Citation: Zhen Yongsu, Li Di,ong, Lin Futian, Li Qian, Tian Peiyu, Xue Yuchuan, , Yang xiaoping. STUDY ON THE ANTITUMOR ACTIVITIES AND THE TOXICITIES OF ZHENGGUANGMYCINS A5 AND A2J. Acta Pharmaceutica Sinica, 1979, 14(2): 83-90.

争光霉素A5和争光霉素A2的抗肿瘤作用与毒性研究

STUDY ON THE ANTITUMOR ACTIVITIES AND THE TOXICITIES OF ZHENGGUANGMYCINS A5 AND A2

  • 摘要: 争光霉素是由浙江平阳分离的链霉菌产生的抗肿瘤物质,是由十多种组分组成的复合物。理化性质研究表明,争光霉素A2、A5、B2等组分与日本报道的博莱霉素(Bleomycin)相应的组分A2、A5、B2等相同。目前国外临床使用的博莱霉素是以A2为主要组分的复合物。我们对A5与A2组分进行了比较研究,结果表明,两者的生物活性有明显差别,主要表现为:(1)对小鼠食管癌(SGA-73)的抑制作用,A6比A2强;(2)在小鼠食管癌组织中的浓度(微生物测定法),A5比A2高;(3)对小鼠肺的损害作用,A5比A2轻;(4)对小鼠的急性毒性,A5比A2低。上述研究结果提示,争光霉素A5是具有一定特点的新抗癌药。最近,单一组分的争光霉素A5定名为平阳霉素。

     

    Abstract: Zhengguangmycin, an antitumor antibiotic complex consisting of more than ten components, is produced by Streptornyces pingyangensis n. sp. isolated from a soil sample collected in Pingyang, Zhejiang province. Two components of zhengguangmycin, namely A2 and A5 were found to be identical with bleomycins A2 and A5 respectively. As bleomycin presently available for clinical use contains bleomycin A2 as its major component, the biological activities of zhengguangmycin A5 were studied in comparison with those of zhengguangmycin A2. The main differences found are as follows; (1) On an equal LD50 basis the inhibitory effect of A5 on transplantable esophageal carcinoma SGA-73 in mice is much stronger than that of A2; (2) The concenrration of A5 attained in the mouse esophageal carcinoma tissue as determined by microbiological assay is much higher than that of A2; (3) As shown by light and electron microscopy A5 appears to be less injurious to the mouse lung than A2 on an equal body weight dosage basis and (4) A5 appears to be less toxic to the mouse in acute toxicity experiments. These results suggest that zhengguangmycin A5 possesses more desirable properties than A2 as an antitumor agent.

     

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