Three new 16-membered macrolide compounds from a genetically engineered strain S. avermitilis MHJ1011

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• 作者：Jun-Jie Pan^a ; ^&dagger ; ; Xu Wan^a ; ^&dagger ; ; Shao-Yong Zhang^a ; Jun Huang^b ; Hui Zhang^b ; An-Liang Chen^a ; ^{anlchen@126.com" class="auth_mail" title="E-mail the corresponding author} ; Ji-Dong Wang^a ; ^b ; ^{jdwang@hisunpharm.com" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Genetically engineered strain S. avermitilis MHJ1011 ; 16-Membered macrolide compounds ; Acaricidal activity
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 July 2016
• 年：2016
• 卷：26
• 期：14
• 页码：3376-3379
• 全文大小：399 K

文摘

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 0.0235 mg/L, respectively, which are higher than those of 13α-hydroxy milbemycin β₃ and 13α-hydroxy-25-ethyl milbemycin β₃.