海洋来源真菌菌株 Penicillium sp. SF-5497 中的新型 preaustinoids 及其对 PTP1B 活性的抑制作用。
New preaustinoids from a marine-derived fungal strain Penicillium sp. SF-5497 and their inhibitory effects against PTP1B activity.
机构信息
College of Pharmacy, Wonkwang University, Iksan, 54538, Republic of Korea.
Institute of Marine Biochemistry, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Cau Giay, Hanoi, Vietnam.
出版信息
J Antibiot (Tokyo). 2019 Aug;72(8):629-633. doi: 10.1038/s41429-019-0187-7. Epub 2019 Apr 24.
Chemical investigation of the marine-derived fungal isolate Penicillium sp. SF-5497 resulted in the isolation of two new preaustinoid-related meroterpenoids, named preaustinoid A6 (1) and preaustinoid A7 (2), along with three known metabolites (3-5). Their structures were elucidated by extensive spectroscopic analyses, such as 1D and 2D NMR and MS data. Among these, compounds 1 and 3 inhibited PTP1B activity in a dose-dependent manner, with IC values of 17.6 and 58.4 µM, respectively. Furthermore, kinetic analyses indicated that compound 1 inhibited PTP1B in a noncompetitive manner, with the K value of 17.0 µM.
海洋来源真菌菌株 Penicillium sp. SF-5497 的化学成分研究分离得到了两个新的 preustinoid 相关的混合萜类化合物，命名为 preaustinoid A6（1）和 preaustinoid A7（2），以及三个已知代谢产物（3-5）。它们的结构通过广泛的光谱分析，如 1D 和 2D NMR 和 MS 数据得到阐明。其中，化合物 1 和 3 以剂量依赖的方式抑制 PTP1B 活性，IC 值分别为 17.6 和 58.4 μM。此外，动力学分析表明化合物 1 以非竞争性方式抑制 PTP1B，K 值为 17.0 μM。
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