Three new 16-membered macrolide compounds from a genetically engineered strain S. avermitilis MHJ1011.
作者信息
Pan Jun-Jie, Wan Xu, Zhang Shao-Yong, Huang Jun, Zhang Hui, Chen An-Liang, Wang Ji-Dong
机构信息
Provincial Joint Engineering Laboratory of Biopesticide Preparation, School of Forestry & Biotechnology, Zhejiang Agricultural and Forestry University, Lin'An 311300, PR China.
Department of New Drug Screening, Zhejiang Hisun Pharmaceutical Co., Ltd, Taizhou 318000, PR China.
出版信息
Bioorg Med Chem Lett. 2016 Jul 15;26(14):3376-3379. doi: 10.1016/j.bmcl.2016.04.033. Epub 2016 May 28.
Three new 16-membered macrolide compounds, 13α-O-α-l-oleandrosyl milbemycin β3 (1), 13α-O-α-l-oleandrosyl-25-ethyl milbemycin β3 (2), 13α-O-α-l-oleandrosyl-25-isopropyl milbemycin β3 (3), were isolated from the genetically engineered strains Streptomyces avermitilis MHJ1011. Their structures were determined on the basis of spectroscopic analysis, including 1D and 2D NMR techniques as well as ESI-MS and comparison with data from the literature. Both compounds 1-3 displayed impressive acaricidal activity against larval mites with the IC50 values of 0.0327, 0.0276 and 0.0235mg/L, respectively, which are higher than those of 13α-hydroxy milbemycin β3 and 13α-hydroxy-25-ethyl milbemycin β3.
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