Bio-Center, Gyeonggido Business & Science Accelerator (GBSA), Suwon 16229, Republic of Korea; Department of Biosystems and Biotechnology, College of Life Sciences and Biotechnology, Korea University, Seoul 02841, Republic of Korea.
Bio-Center, Gyeonggido Business & Science Accelerator (GBSA), Suwon 16229, Republic of Korea.
Bioorg Chem. 2019 Jun;87:714-719. doi: 10.1016/j.bioorg.2019.03.069. Epub 2019 Mar 28.
The ethanolic extract obtained from the stems of Glycosmis pentaphylla was found to suppress antigen-mediated degranulation of rat basophilic leukemia (RBL-2H3) cells. Four new geranylated 2-quinolone alkaloids, named glycopentanolones A-D (1-4), and 12 known metabolites (5-16) were isolated from the ethanolic extract from the stems of G. pentaphylla using bioassay-guided fractionation. Their structures were elucidated by a combination of 1D and 2D NMR, and HRESI-MS. The inhibitory effects of the isolated constituents on β-hexosaminidase release from RBL-2H3 cells were examined, and compounds 1, 5, 8 and 11 exhibited potent inhibitory activity with IC values between 0.05 and 4.28 μM.
从五叶瓜藤的茎中获得的乙醇提取物被发现可抑制大鼠嗜碱性白血病（RBL-2H3）细胞的抗原介导的脱粒。从五叶瓜藤的乙醇提取物中，通过生物测定指导的分级分离，分离出四种新的香叶基化 2-喹诺酮生物碱，命名为 glycopentanolones A-D（1-4）和 12 种已知代谢物（5-16）。通过 1D 和 2D NMR 以及 HRESI-MS 的组合，阐明了它们的结构。对分离出的成分对 RBL-2H3 细胞β-己糖胺酶释放的抑制作用进行了检查，化合物 1、5、8 和 11 表现出很强的抑制活性，IC 值在 0.05 和 4.28 μM 之间。
