许鸿章, 张鹤镛. 平阳霉素的分离和鉴别J. 药学学报, 1980, 15(10): 609-614.
引用本文: 许鸿章, 张鹤镛. 平阳霉素的分离和鉴别J. 药学学报, 1980, 15(10): 609-614.
Xu Hongzhang Zhang Heyong, . THE ISOLATION AND IDENTIFICATION OF PINGYANGMYCINJ. Acta Pharmaceutica Sinica, 1980, 15(10): 609-614.
Citation: Xu Hongzhang Zhang Heyong, . THE ISOLATION AND IDENTIFICATION OF PINGYANGMYCINJ. Acta Pharmaceutica Sinica, 1980, 15(10): 609-614.

平阳霉素的分离和鉴别

THE ISOLATION AND IDENTIFICATION OF PINGYANGMYCIN

  • 摘要: 轮枝链霉菌平阳新变种(Str.Verticillus Vat.Pingyangensis n.Var.)所产生的抗肿瘤抗菌素是由十余种组分组成的复合物,其中两个主要组分分别与博莱霉素A2和B2完全相同。在生产过程中通过菌种选育和发酵工艺的改进,产品的组成发生了变化,主要组分变成了博莱霉素A5,已正式命名为平阳霉素。它在复合物中所占比例一般约为60%。本文报告平阳霉素的分离、理化性质和鉴别。

     

    Abstract: Zhengguangmycin, an antitumor antibiotic complex consisting of more than ten components, is produced by str. Verticillus vat pingyangensis n. var. As reported previously, two major components of this complex are A2 and B2. However, during the course of its manufacture a change has taken place in the constitution of the zhengguangmycin complex, the predominant component obtained from CM-sephadex-C-25 column chromatography was found to correspond to zhengguangmycin A5 according to its elution sequence. This component was isolated and purified, and was named pingyangmycin. Based on its physicochemical properties, the results of comparison of its terminal amine moiety with spermidine and 13C NMR spectrum analysis, the identity of this component. with bleomycin A5 was confirmed. In comparison with zhengguangmycin A2 (in mice), pingyangmycin appeared to be less toxic in acute toxicity experiments and less injurious to the lung, a much higher concentration was attained in the esophageal carcinoma tissue and a much stronger inhibitory effect was obtained against transplantable esophageal carcinoma SGA-73. Clinical studies in 349 cases of various kinds of cancer showed that pengyangmycin was markedly effective against squamous cell carcinoma of the head, neck and the cervix and fairly effective against mammary, nasopharyngeal and esophageal carcinoma. In View of the fact that bleomycin obtained from commercial sources contains A2 as its main component with only trace amount of bleomycin A5, pingyangmycin would be more interesting as an antitumor agent. This paper deals with the results of isolation, physicochemical properties and identification of pingyangmycin.

     

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