海洋来源的 Tunicamycins 通过抑制 MurNAc-Pentapeptide 转位酶发挥作用。
Tunicamycins from Marine-Derived Inhibit MurNAc-Pentapeptide Translocase in .
机构信息
Department of Agricultural Biotechnology, College of Agriculture and Life Sciences and Natural Products Research Institute, Seoul National University, Seoul 08826, Republic of Korea.
Natural Products Research Institute, College of Pharmacy, Seoul National University, Seoul 08826, Republic of Korea.
出版信息
Mar Drugs. 2024 Jun 26;22(7):293. doi: 10.3390/md22070293.
Four tunicamycin class compounds, tunicamycin VII (), tunicamycin VIII (), corynetoxin U17a (), and tunicamycin IX (), were isolated from the culture broth of the marine-derived actinomycete sp. MBTG32. The strain was identified using the 16S rDNA sequencing technique, and the isolated strain was closely related to . The structures of the isolated compounds were elucidated based on spectroscopic data and comparisons with previously reported NMR data. Compounds - showed potent antibacterial activities against Gram-positive bacteria, especially with MIC values of 0.13-0.25 µg/mL. Through a recombinant enzyme assay and overexpression analysis, we found that the isolated compounds exerted potent inhibitory effects on MurNAc-pentapeptide translocase (MraY), with IC values of 0.08-0.21 µg/mL. The present results support that the underlying mechanism of action of tunicamycins isolated from marine-derived sp. is also associated with the inhibition of MraY enzyme activity in .
从海洋来源放线菌 sp. MBTG32 的发酵液中分离得到了 4 种衣霉素类化合物，包括衣霉素 VII()、衣霉素 VIII()、棒曲霉素 U17a()和衣霉素 IX()。通过 16S rDNA 测序技术对该菌株进行了鉴定，分离出的菌株与 密切相关。根据光谱数据和与先前报道的 NMR 数据的比较，解析了分离化合物的结构。化合物 - 对革兰氏阳性菌表现出很强的抗菌活性，特别是对 的 MIC 值为 0.13-0.25 µg/mL。通过重组酶测定和过表达分析，我们发现分离出的化合物对 MurNAc-五肽转位酶（MraY）表现出很强的抑制作用，IC 值为 0.08-0.21 µg/mL。这些结果表明，来源于海洋来源 sp. 的衣霉素的作用机制也与抑制 MraY 酶活性有关。
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