Graduate School of Life Science, Hokkaido University, Sapporo 001-0021, Japan.
Faculty of Advanced Life Science, Hokkaido University, Sapporo 001-0021, Japan.
Molecules. 2020 Sep 7;25(18):4077. doi: 10.3390/molecules25184077.
Species of the genus have been used in traditional Chinese medicine, with the medicinal herb "Manshanfong" used as an expectorant and for the treatment of acute bronchitis. Daurichromenic acid (DCA), a constituent of , is a meroterpenoid with antibacterial, anti-HIV, and anti-inflammatory activities. However, the mechanisms underlying these pharmacologic activities are poorly understood. To develop new drugs based on DCA, more information is required regarding its interactions with biomolecules. The present study showed that DCA inhibits the activity of the enzyme sphingomyelin synthase, with an IC of 4 µM. The structure-activity relationships between DCA and sphingomyelin synthase were evaluated using derivatives and cyclized hongoquercin A. In addition, DCA was found to inhibit amyloid β aggregation. These results may help in the design of effective drugs based on DCA.
已在传统中药中使用 属的物种，药用植物“满山丰”用作祛痰药和治疗急性支气管炎。道利色烯酸（DCA）是 的一种倍半萜烯，具有抗菌、抗 HIV 和抗炎活性。然而，这些药理活性的机制尚不清楚。为了基于 DCA 开发新药，需要更多关于其与生物分子相互作用的信息。本研究表明，DCA 抑制神经鞘磷脂合酶的活性，IC 为 4 µM。使用衍生物和环化的红曲曲菌素 A 评估了 DCA 与神经鞘磷脂合酶之间的构效关系。此外，还发现 DCA 可抑制淀粉样β聚集。这些结果可能有助于基于 DCA 设计有效的药物。
