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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 20期

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

页码：5710 / 5713

页数：4