Umezawa H
Biomedicine. 1977 Jul;26(4):236-49.
Antibiotics and small molecular enzyme inhibitors produced by micro-organisms are microbial secondary metabolites which have no obvious function in the growth of microorganisms. Involvement of plasmids in their biosyntheses has been studied and the structure of the microbial world where various compounds with widely varying structures have been found has been shown to be due to the presence of a great variety of plasmids. On the basis of this structure of microbial world, the author has found the microbial products which have various activities useful in treatment of cancer or in suppression of carcinogenesis. In this paper, the author reviewed his following studies: the plasmid involvement in biosyntheses of bioactive microbial secondary metabolites; the mechanism of therapeutic effect of bleomycin, and the development of useful analogs and derivatives of bleomycin and anthracyclic antibiotics; the screening method to find compounds affecting immune system, and the action of bestatin in enhancing delayed-type hypersensitivity and therapeutic effects of anticancer agents; enzyme inhibitors with potential utility in treatment or prevention of cancer.
微生物产生的抗生素和小分子酶抑制剂是微生物的次级代谢产物,它们在微生物生长过程中没有明显功能。人们已经研究了质粒在它们生物合成中的作用,并且发现存在各种结构差异很大的化合物的微生物世界的结构已被证明是由于存在各种各样的质粒。基于微生物世界的这种结构,作者发现了对癌症治疗或致癌作用抑制具有各种有用活性的微生物产物。在本文中,作者回顾了他的以下研究:质粒参与生物活性微生物次级代谢产物的生物合成;博来霉素的治疗作用机制,以及博来霉素和蒽环类抗生素的有用类似物和衍生物的开发;寻找影响免疫系统的化合物的筛选方法,以及贝他汀在增强迟发型超敏反应和抗癌药物治疗效果方面的作用;在癌症治疗或预防中具有潜在用途的酶抑制剂。