Department of Oncology, Hematology and Bone Marrow Transplantation with Section Pneumology, Hubertus Wald-Tumorzentrum, University Medical Center Hamburg-Eppendorf, 20251 Hamburg, Germany.
Laboratory of Biologicaly Active Compounds, School of Natural Sciences, Far Eastern Federal University, Vladivostok 690091, Russia.
Biomolecules. 2020 Mar 14;10(3):451. doi: 10.3390/biom10030451.
From a root bark of Turch we isolated two new (7 and 8) and six previously known compounds (1-6) belonging to the group of prenylated polyphenols. Their structures were elucidated using mass spectrometry, nuclear magnetic resonance and circular dichroism spectroscopy. These natural compounds selectively inhibited human drug-resistant prostate cancer in vitro. Prenylated pterocarpans 1-3 prevented the cell cycle progression of human cancer cells in S-phase. This was accompanied by a reduced expression of mRNA corresponding to several human cyclin-dependent kinases (CDKs). In contrast, compounds 4-8 induced a G1-phase cell cycle arrest without any pronounced effect on CDKs mRNA expression. Interestingly, a non-substituted hydroxy group at C-8 of ring D of the pterocarpan skeleton of compounds 1-3 seems to be important for the CDKs inhibitory activity.
从 Turch 的根皮中,我们分离出两种新的(7 和 8)和六种以前已知的化合物(1-6),它们属于类异戊烯基多酚。利用质谱、核磁共振和圆二色性光谱法阐明了它们的结构。这些天然化合物在体外选择性地抑制了人耐药前列腺癌。类异戊烯基紫檀烷 1-3 阻止了人癌细胞在 S 期的细胞周期进展。这伴随着对应于几种人细胞周期蛋白依赖性激酶(CDKs)的 mRNA 表达减少。相比之下,化合物 4-8 诱导 G1 期细胞周期停滞,而对 CDK mRNA 表达没有明显影响。有趣的是,化合物 1-3 中紫檀烷骨架的 D 环 C-8 位的非取代羟基似乎对 CDK 抑制活性很重要。