New nemadectin congeners with acaricidal and nematocidal activity from Streptomyces microflavus neau3 Y-3

被引:19
作者
Yang, Ling-Yu [1 ]
Wang, Ji-Dong [2 ]
Zhang, Ji [1 ]
Xue, Chang-Yan [1 ]
Zhang, Hui [2 ]
Wang, Xiang-Jing [2 ]
Xiang, Wen-Sheng [1 ]
机构
[1] Northeast Agr Univ, Sch Life Sci, Harbin 150030, Peoples R China
[2] Zhejiang Hisun Pharmaceut Co Ltd, Taizhou 318000, Peoples R China
基金
中国国家自然科学基金;
关键词
Nemadectin congeners; Acaricidal activity; Nematocidal activity; Streptomyces microflavus neau3; STRUCTURE ELUCIDATION; BIOLOGICAL-ACTIVITIES; AVERMITILIS NEAU1069; NATURAL-PRODUCTS; FERMENTATION; MILBEMYCINS; IVERMECTIN; PROTECTION; FAMILY;
D O I
10.1016/j.bmcl.2013.08.002
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Two nemadectin congeners 1 and 2 were isolated from the fermentation broth of a mutant strain (Y-3) of Streptomyces microflavus neau3. Their structures were determined on the basis of extensive spectroscopic analysis and comparison with data from the literature. Compound 2 possessed a 5-membered ring lactone that is unprecedented among known milbemycins and avermectins. Both compounds 1 and 2 exhibited potent acaricidal activity and nematocidal activity. Especially, compound 2 demonstrated impressive acaricidal activity against adult mites with an IC50 of 2.3 +/- 0.9 mu g/mL and mite eggs with an IC50 of 17.5 +/- 2.1 mu g/mL and nematocidal activity against Caenorhabditis elegans with an IC50 of 0.7 +/- 0.2 mu g/mL, which are higher than those of nemadectin and the known commercial acaricide and nematocide milbemycin A3/A4. (C) 2013 Elsevier Ltd. All rights reserved.
引用
收藏
页码:5710 / 5713
页数:4
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