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沙普里霉素,由链霉菌产生的新型抗肿瘤抗生素。产生菌、发酵、分离及生物学特性。

Sapurimycin, new antitumor antibiotic produced by Streptomyces. Producing organism, fermentation, isolation and biological properties.

作者信息

Hara M, Takiguchi T, Ashizawa T, Gomi K, Nakano H

机构信息

Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Japan.

出版信息

J Antibiot (Tokyo). 1991 Jan;44(1):33-9. doi: 10.7164/antibiotics.44.33.

Abstract

In screening actinomycetes for antitumor compounds, Streptomyces sp. DO-116 was found to produce a new antitumor antibiotic sapurimycin. It is structurally related to, but distinct from, kapurimycins. The antibiotic was produced in a fermentation medium supplemented with high porous polymer resin which adsorbs antibiotic in the culture and results in an increase of titer. Active material was separated from the polymer resin by a solvent extraction procedure and isolated by repeated solvent extraction, adsorption chromatography and HPLC. Sapurimycin was active against bacteria, particularly Gram-positive organisms. It exhibited antitumor activity against leukemia P388 and sarcoma 180 in mice. Sapurimycin caused single strand breaks in supercoiled plasmid DNA in vitro. These results are discussed in comparison with data for kapurimycins.

摘要

在筛选放线菌以寻找抗肿瘤化合物的过程中,发现链霉菌属DO-116能产生一种新的抗肿瘤抗生素沙普霉素。它在结构上与卡普霉素相关,但又有所不同。该抗生素是在添加了高孔隙率聚合物树脂的发酵培养基中产生的,这种树脂能吸附培养物中的抗生素,从而提高效价。通过溶剂萃取法从聚合物树脂中分离出活性物质,并通过反复溶剂萃取、吸附色谱和高效液相色谱进行分离。沙普霉素对细菌有活性,尤其是革兰氏阳性菌。它对小鼠白血病P388和肉瘤180具有抗肿瘤活性。沙普霉素在体外能导致超螺旋质粒DNA产生单链断裂。将这些结果与卡普霉素的数据进行了比较讨论。

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