从 Acer nikoense 中分离得到的作为 Na+-葡萄糖协同转运蛋白 (SGLT) 抑制剂的环状二芳基庚烷类化合物。
Cyclic diarylheptanoids as Na+-glucose cotransporter (SGLT) inhibitors from Acer nikoense.
机构信息
Faculty of Pharmaceutical Sciences, Hoshi University, Ebara 2-4-41 Shinagawa-ku, Tokyo 142-8501, Japan.
出版信息
Bioorg Med Chem Lett. 2010 Feb 1;20(3):1070-4. doi: 10.1016/j.bmcl.2009.12.036. Epub 2009 Dec 11.
Two cyclic diarylheptanoids, acerogenins A (1) and B (2) have been isolated from the bark of Acer nikoense as inhibitors of Na(+)-glucose cotransporter (SGLT). Acerogenins A (1) and B (2) inhibited both isoforms, SGLT1 and SGLT2. Structure-activity relationship of acerogenin derivatives on inhibitory activity of SGLT as well as conformational analysis of 1 and 2 on the basis of J-resolved HMBC spectra and X-ray analysis were discussed.
从 Acer nikoense 的树皮中分离得到两种环状二芳基庚烷类化合物，acerogenins A（1）和 B（2），它们是 Na(+)-葡萄糖共转运蛋白（SGLT）的抑制剂。Acerogenins A（1）和 B（2）抑制了 SGLT 的两种同工酶，SGLT1 和 SGLT2。根据 J 分辨 HMBC 光谱和 X 射线分析，讨论了 acerogenin 衍生物对 SGLT 抑制活性的构效关系，以及 1 和 2 的构象分析。
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