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新型米尔贝肟类似物来源于微黄色链霉菌新 3 号:发酵、分离、结构鉴定和生物活性。

New nemadectin congener from Streptomyces microflavus neau3: fermentation, isolation, structure elucidation and biological activities.

机构信息

School of Life Science, Northeast Agricultural University, Harbin, PR China.

出版信息

J Antibiot (Tokyo). 2010 Apr;63(4):171-5. doi: 10.1038/ja.2010.12. Epub 2010 Feb 26.

Abstract

Bioactivity-guided fractionation of Streptomyces microflavus neau3 fermentation broth was used to determine the chemical identity of bioactive constituents. The structure of the new compound 1 was determined on the basis of spectroscopic analysis, including 1D and 2D NMR, as well as HRESI-MS, ESI-MS, UV and IR, and compared with the data reported in the literature. The acaricidal and nematocidal activities of the isolated compound 1 and its previously reported analogs 2, 3, 4 and 5 were evaluated. The results demonstrate that compounds 1, 2, 3, 4 and 5, especially compound 1, have potential as antiparasitics with acaricidal and nematocidal activities. These lactones shed new insights into the structural diversity of nemadectin and milbemycin analog libraries that are potentially accessible by combinatorial biosynthesis.

摘要

采用生物活性导向的方法对链霉菌发酵液进行分离,以确定生物活性成分的化学结构。根据光谱分析,包括 1D 和 2D NMR、HRESI-MS、ESI-MS、UV 和 IR,确定了新化合物 1 的结构,并与文献报道的数据进行了比较。对分离得到的化合物 1 及其先前报道的类似物 2、3、4 和 5 的杀螨和杀线虫活性进行了评估。结果表明,化合物 1、2、3、4 和 5,特别是化合物 1,具有作为杀螨和杀线虫活性的驱虫剂的潜力。这些内酯类化合物为通过组合生物合成获得的拟南芥内酯和米尔贝霉素类似物文库的结构多样性提供了新的见解。

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