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二色胡枝子根皮中的多酚类化合物通过诱导细胞凋亡和细胞周期阻滞抑制人前列腺癌细胞的进展。

Polyphenolic Compounds from Lespedeza Bicolor Root Bark Inhibit Progression of Human Prostate Cancer Cells via Induction of Apoptosis and Cell Cycle Arrest.

机构信息

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.

出版信息

Biomolecules. 2020 Mar 14;10(3):451. doi: 10.3390/biom10030451.

Abstract

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/897d/7175281/18a941559fe7/biomolecules-10-00451-g001a.jpg

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