GSK-3β inhibitory activities of novel dichroloresorcinol derivatives from Cosmospora vilior isolated from a mangrove plant
GSK-3β inhibitory activities of novel dichroloresorcinol derivatives from Cosmospora vilior isolated from a mangrove plant
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DOI：
10.1016/j.phytol.2016.09.007
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发表时间：
2016-12-01
影响因子：
1.7
通讯作者：
Kimura, Ken-ichi
中科院分区：
文献类型：
--
作者：
Shiono, Yoshihito;Miyazaki, Nozomi;Kimura, Ken-ichi
Cosmolorins A (1)、B (2) 和 C (3) 是从内生真菌 Cosmospora vilior IM2-155 中分离出来的。通过广泛的光谱分析（包括广泛的 2D NMR、HRESITOFMS 和化学反应）的结合，阐明了 1、2 和 3 的结构。评估了化合物1、2和3的生物活性。化合物1和2部分恢复了突变酵母中Ca2+信号过度激活引起的生长抑制，并显示出糖原合酶激酶(GSK)-3b抑制活性，IC50值分别为62.5和60.6μM。此外，与单独的核因子-kB配体受体激活剂（RANKL）相比，化合物2在RAW264.7细胞中显着增加破骨细胞形成超过1.5倍。 (C) 2016 年欧洲植物化学协会。由爱思唯尔有限公司出版。保留所有权利。
Cosmochlorins A (1), B (2), and C (3) were isolated from the endophytic fungus Cosmospora vilior IM2-155. The structures of 1, 2, and 3 were elucidated by a combination of extensive spectroscopic analyses, including extensive 2D NMR, HRESITOFMS, and chemical reactions. Compounds 1, 2, and 3 were evaluated for their biological activity. Compounds 1 and 2 partially restored the growth inhibition caused by hyperactivated Ca2+-signaling in mutant yeast and showed glycogen synthase kinase (GSK)-3b inhibition activity at IC50 values of 62.5 and 60.6 mu M, respectively. Further, compound 2 significantly increased osteoclast formation by more than 1.5-fold in RAW264.7 cells compared to receptor activator of nuclear factor-kB ligand (RANKL) alone. (C) 2016 Phytochemical Society of Europe. Published by Elsevier Ltd. All rights reserved.