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

Publication date: December 2016 Source:Phytochemistry Letters, Volume 18 Author(s): Yoshihito Shiono, Nozomi Miyazaki, Tetsuya Murayama, Takuya Koseki, Harizon, Dewa Gede Katja, Unang Supratman, Juri Nakata, Yoshito Kakihara, Makio Saeki, Jun Yoshida, Shota Uesugi, Ken-ichi Kimura 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)-3β inhibition activity at IC50 values of 62.5 and 60.6μM, 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-κB ligand (RANKL) alone. Graphical abstract

Source: Phytochemistry Letters - September 30, 2016 Category: Chemistry Source Type: research