来源于海洋真菌菌株 sp. SF-5929 的蛋白酪氨酸磷酸酶 1B 抑制剂。
Protein tyrosine phosphatase 1B inhibitors from a marine-derived fungal strain sp. SF-5929.
机构信息
College of Pharmacy, Wonkwang University, Iksan, Republic of Korea.
College of Medical and Life Sciences, Silla University, Busan, Republic of Korea.
出版信息
Nat Prod Res. 2020 Mar;34(5):675-682. doi: 10.1080/14786419.2018.1499629. Epub 2018 Nov 16.
In the course of our continuing investigation of bioactive secondary metabolites from marine-derived fungal strains, a racemate of a novel diphenolic derivative named (±)-tylopilusin D () along with ten previously known secondary metabolites () were isolated from a marine-derived fungal strain sp. SF-5929. Their structures were elucidated mainly by analysis of NMR and MS data. In addition, the inhibitory effects of the isolated compounds against protein tyrosine phosphatase 1B (PTP1B) activity were evaluated, and compounds , , and inhibited PTP1B activity with IC values ranging from 3.3 to 8.1 µM. Kinetics studies suggested that compounds , , and had noncompetitive inhibitory effects against PTP1B.
在我们对海洋来源真菌菌株中生物活性次生代谢产物的持续研究过程中，从海洋来源真菌菌株 sp. SF-5929 中分离得到了一种新型二酚衍生物的外消旋体（±）-tylopilusin D () 以及十个先前已知的次生代谢产物 ()。它们的结构主要通过 NMR 和 MS 数据分析来阐明。此外，还评价了分离得到的化合物对蛋白酪氨酸磷酸酶 1B（PTP1B）活性的抑制作用，化合物 、 、 对 PTP1B 活性的抑制作用，IC 值范围为 3.3 至 8.1μM。动力学研究表明，化合物 、 、 对 PTP1B 具有非竞争性抑制作用。
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