克拉多孢子菌 A，一种新型蛋白酪氨酸磷酸酶 1B 抑制剂，由印度尼西亚海洋海绵源克拉多孢子菌产生。
Cladosporamide A, a new protein tyrosine phosphatase 1B inhibitor, produced by an Indonesian marine sponge-derived Cladosporium sp.
机构信息
Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, Sendai, 981-8558, Japan.
Faculty of Mathematic and Natural Sciences, Sam Ratulangi University, Kampus Bahu, Manado, 95115, Indonesia.
出版信息
J Nat Med. 2018 Jun;72(3):779-783. doi: 10.1007/s11418-018-1193-y. Epub 2018 Mar 5.
Cladosporamide A (1), a new protein tyrosine phosphatase (PTP) 1B inhibitor, was isolated together with a known prenylated flavanone derivative (2) from the culture broth of an Indonesian marine sponge-derived Cladosporium sp. TPU1507 by solvent extraction, ODS column chromatography, and preparative HPLC (ODS). The structure of 1 was elucidated based on 1D and 2D NMR data. Compound 1 modestly inhibited PTP1B and T-cell PTP (TCPTP) activities with IC values of 48 and 54 μM, respectively. The inhibitory activity of 2 against PTP1B (IC = 11 μM) was approximately 2-fold stronger than that against TCPTP (IC = 27 μM).
克拉多孢子素 A（1）是一种新型的蛋白酪氨酸磷酸酶（PTP）1B 抑制剂，从印度尼西亚海洋海绵来源的 Cladosporium sp. TPU1507 的发酵液中通过溶剂萃取、ODS 柱层析和制备型 HPLC（ODS）分离得到，同时还分离得到了一个已知的被prenylated flavanone 衍生物（2）。1 的结构根据 1D 和 2D NMR 数据确定。化合物 1 对 PTP1B 和 T 细胞 PTP（TCPTP）的活性具有中等抑制作用，IC 值分别为 48 和 54 μM。2 对 PTP1B 的抑制活性（IC = 11 μM）大约比 TCPTP（IC = 27 μM）强两倍。
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