GSK-3 beta inhibitory activities of novel dichroloresorcinol derivatives from Cosmospora vilior isolated from a mangrove plant

作者:Shiono Yoshihito*; Miyazaki Nozomi; Murayama Tetsuya; Koseki Takuya; Harizon; Katja Dewa Gede; Supratman Unang; Nakata Juri; Kakihara Yoshito; Saeki Makio; Yoshida Jun; Uesugi Shota; Kimura Ken ichi
来源:Phytochemistry Letters, 2016, 18: 122-127.
DOI:10.1016/j.phytol.2016.09.007

摘要

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.

  • 出版日期2016-12