海洋放线菌 ACT232 来源的乳链菌肽 A-C，一种抑制组织蛋白酶 B 的去磷酸化磷酰化乳链菌肽衍生物。
Lactomycins A-C, Dephosphorylated Phoslactomycin Derivatives that Inhibit Cathepsin B, from the Marine-derived Streptomyces sp. ACT232.
机构信息
Laboratory of Aquatic Natural Products Chemistry, Graduate School of Agricultural and Life Sciences, The University of Tokyo, Tokyo 113-8657, Japan.
Laboratory of Aquatic Molecular Biology and Biotechnology, Graduate School of Agricultural and LifeSciences, The University of Tokyo, Tokyo 113-8657, Japan.
出版信息
Mar Drugs. 2018 Feb 21;16(2):70. doi: 10.3390/md16020070.
Three new polyketides, lactomycins A (1)-C (3), were isolated from the culture broth of a marine-derived sp. ACT232 as cathepsin B inhibitors. Their structures were determined by a combination of NMR and MS data analyses to be the dephosphorylated derivatives of a phoslactomycin class of metabolites. Lactomycins exhibited cathepsin B inhibitory activity (IC50 0.8 to 4.5 μg/mL). Even though the biosynthetic gene clusters found in the genome of the current strain have high similarity to those of phoslactomycin, neither phoslactomycins nor leustroducsins were detected by LC-MS analyses of the crude extract.
从海洋来源的 sp. ACT232 的发酵液中分离到三种新的聚酮化合物，乳霉素 A（1）-C（3），它们是组织蛋白酶 B 的抑制剂。通过 NMR 和 MS 数据分析的组合确定了它们的结构，它们是磷酸乳霉素类代谢物的去磷酸化衍生物。乳霉素表现出组织蛋白酶 B 抑制活性（IC50 为 0.8 至 4.5 μg/mL）。尽管当前菌株基因组中发现的生物合成基因簇与磷酸乳霉素的基因簇高度相似，但通过对粗提物进行 LC-MS 分析，既未检测到磷酸乳霉素，也未检测到 leustroducsin。
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