通过核磁共振指纹图谱分析鉴定出的来自细脉海桐的LAT转运抑制剂。
LAT Transport Inhibitors from Pittosporum venulosum Identified by NMR Fingerprint Analysis.
作者信息
Grkovic Tanja, Pouwer Rebecca H, Wang Qian, Guymer Gordon P, Holst Jeff, Quinn Ronald J
机构信息
†Eskitis Institute for Drug Discovery, Griffith University, Brisbane, QLD 4111, Australia.
⊥Sydney Medical School, University of Sydney, Sydney, NSW 2006, Australia.
出版信息
J Nat Prod. 2015 Jun 26;78(6):1215-20. doi: 10.1021/np500968t. Epub 2015 May 18.
(1)H NMR fingerprints were used as the guiding principle for the isolation of minor compounds related to the l-type amino acid transporter inhibitors venulosides A (1) and B (2). Two new monoterpene glycosides, namely, venulosides C (3) and D (4), were isolated from a Queensland collection of the plant Pittosporum venulosum. Compounds 3 and 4 were found to inhibit l-leucine transport in LNCaP cells with IC50 values of 11.47 and 39.73 μM, respectively. The venulosides are the first reported natural product inhibitors of leucine transport in prostate cancer cells, and the isolation of the minor compounds provides some early SAR information.
（1）¹H NMR指纹图谱被用作分离与l型氨基酸转运体抑制剂venulosides A（1）和B（2）相关的次要化合物的指导原则。从昆士兰采集的小叶海桐（Pittosporum venulosum）植物中分离出两种新的单萜糖苷，即venulosides C（3）和D（4）。发现化合物3和4可抑制LNCaP细胞中的l-亮氨酸转运，IC50值分别为11.47和39.73 μM。venulosides是首次报道的前列腺癌细胞中亮氨酸转运的天然产物抑制剂，次要化合物的分离提供了一些早期的构效关系信息。
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