大环内酰胺类：由马杜拉放线菌SCC 1776和SCC 1777产生的一类新型抗真菌抗生素。

Macrolactams: a novel class of antifungal antibiotics produced by Actinomadura spp. SCC 1776 and SCC 1777.

作者信息

Hegde V, Patel M, Horan A, Gullo V, Marquez J, Gunnarsson I, Gentile F, Loebenberg D, King A, Puar M

机构信息

Microbial Products, Schering-Plough Research, Bloomfield, NJ 07003.

出版信息

J Antibiot (Tokyo). 1992 May;45(5):624-32. doi: 10.7164/antibiotics.45.624.

DOI:10.7164/antibiotics.45.624

PMID:1624364

Abstract

Three novel antifungal antibiotics, Sch 38518, Sch 39185 and Sch 38516 were isolated from the fermentation broths of two actinomycetes identified by chemical, morphological and physiological analysis as a new species of Actinomadura. The compounds were isolated from broth by solvent extraction and purified by silica gel chromatography. Physico-chemical properties, mass spectral analysis, IR and UV suggested the compounds were similar. Sch 38518 and Sch 39185 have a molecular formula of C25H48N2O5. 1H NMR, 13C NMR and hydrolysis indicated the aglycones were identical, however the compounds differed in containing isomeric sugar moieties. Sch 38518 contains mycosamine while Sch 39185 contains 3,6-dideoxy-3-amino-L-talopyranose. Sch 38516 has a molecular formula of C24H46N2O5 and is a lower homolog of Sch 39185. The three compounds, Sch 38518 (1), Sch 39185 (2), and Sch 38516 (3) exhibit similar activity against Candida spp. with geometric mean MICs of 1.81, 2.00 and 0.91 micrograms/ml, respectively.

摘要

从两种放线菌的发酵液中分离出三种新型抗真菌抗生素，即Sch 38518、Sch 39185和Sch 38516。通过化学、形态学和生理学分析，这两种放线菌被鉴定为马杜拉放线菌属的一个新物种。这些化合物通过溶剂萃取从发酵液中分离出来，并通过硅胶柱色谱法进行纯化。物理化学性质、质谱分析、红外光谱和紫外光谱表明这些化合物相似。Sch 38518和Sch 39185的分子式为C25H48N2O5。1H核磁共振、13C核磁共振和水解分析表明其苷元相同，但这两种化合物所含的糖部分为异构体。Sch 38518含有肌醇胺，而Sch 39185含有3,6 -二脱氧-3-氨基-L-塔罗吡喃糖。Sch 38516的分子式为C24H46N2O5，是Sch 39185的低级同系物。这三种化合物，即Sch 38518（1）、Sch 39185（2）和Sch 38516（3）对念珠菌属表现出相似的活性，几何平均最小抑菌浓度分别为1.81、2.00和0.91微克/毫升。