从红树林来源的链霉菌 SCSIO ZJ89 中分离得到的具有细胞毒性和抑制细胞迁移的博莱霉素 F-I。
Borrelidins F-I, cytotoxic and cell migration inhibiting agents from mangrove-derived Streptomyces rochei SCSIO ZJ89.
机构信息
CAS Key Laboratory of Tropical Marine Bio-resources and Ecology, Guangdong Key Laboratory of Marine Materia Medica, RNAM Center for Marine Microbiology, South China Sea Institute of Oceanology, Chinese Academy of Sciences, 164 West Xingang Road, Guangzhou 510301, China; College of Bioengineering, Chongqing UniversIty, Chongqing 400044, China.
Guangdong Provincial Key Laboratory of Medical Molecular Diagnostics, Institute of Laboratory Medicine, Dongguan Key Laboratory of Environmental Medicine, Guangdong Medical University, No. 1 Xincheng Road, Dongguan 523808, China.
出版信息
Bioorg Med Chem. 2018 May 1;26(8):1488-1494. doi: 10.1016/j.bmc.2018.01.010. Epub 2018 Feb 7.
Borrelidin A (1) is produced by several species of Streptomyces and within its bioactive scaffold, the vinylic nitrile moiety is essential for activity. We report herein newly discovered members of the borrelidin family, borrelidin F (2), borrelidin G (3), borrelidin H (4) and borrelidin I (5); all were isolated from Streptomyces rochei SCSIO ZJ89 originating from a mangrove-derived sediment sample. These structurally diverse metabolites enabled a number of new structure-activity relationships (SARs) to be identified, especially with respect to the different configurations at the C11-OH and C12-C15 double bonds for which the absolute configurations were determined using spectroscopic methods. Importantly, borrelidin H (4) was found to have a therapeutic window superior to that of borrelidin A (1) in vitro and could inhibit migration of cancer cells.
布雷菲德菌素 A（1）由几种链霉菌产生，在其生物活性支架内，乙烯基腈部分对于活性是必不可少的。我们在此报告布雷菲德菌素家族的新发现成员，布雷菲德菌素 F（2）、布雷菲德菌素 G（3）、布雷菲德菌素 H（4）和布雷菲德菌素 I（5）；它们均从红树林来源的沉积物样本中分离得到的链霉菌罗氏 SCSIO ZJ89 中分离得到。这些结构多样的代谢产物使许多新的结构-活性关系（SAR）得以确定，特别是对于 C11-OH 和 C12-C15 双键的不同构型，其绝对构型是使用光谱方法确定的。重要的是，发现布雷菲德菌素 H（4）在体外具有优于布雷菲德菌素 A（1）的治疗窗，可以抑制癌细胞的迁移。
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