Department of Pharmacy Engineering, Tianjin University of Technology, Tianjin, 300384, PR China.
Department of Pharmacy Engineering, Tianjin University of Technology, Tianjin, 300384, PR China; Tianjin Key Laboratory of Drug Targeting and Bioimaging, Tianjin University of Technology, Tianjin, 300384, PR China.
Phytochemistry. 2022 Sep;201:113279. doi: 10.1016/j.phytochem.2022.113279. Epub 2022 Jun 18.
Four undescribed and five known isosteroidal alkaloids were isolated from the bulbs of Fritillaria taipaiensis and their structures were elucidated on the basis of HR-ESI-MS, 1D and 2D NMR spectroscopic data analyses. The undescribed compounds were designated taipainines A-D. Of these, taipainine D presented a unique structure having the D/E trans (H-13α/H-17β) and E/F cis (β-axial lone pair of the N atom/H-22β) ring junctions. Possible biosynthetic pathway to taipainine D is proposed. Four compounds showed significant BChE inhibitory activities similar or better than the positive control galantamine. In addition, the preliminary structure-activity relationships (SARs) of these isosteroidal alkaloids were also investigated.
从太白贝母鳞茎中分离得到四个未见报道的和五个已知的同型甾体生物碱，并根据高分辨电喷雾质谱（HR-ESI-MS）、一维和二维核磁共振（1D 和 2D NMR）波谱数据分析它们的结构。这些未见报道的化合物被命名为太白贝母碱 A-D。其中，太白贝母碱 D 具有独特的结构，其 D/E 反式（H-13α/H-17β）和 E/F 顺式（β-轴向氮原子的孤对电子/H-22β）环连接。提出了太白贝母碱 D 的可能生物合成途径。四种化合物表现出显著的乙酰胆碱酯酶（BChE）抑制活性，与阳性对照加兰他敏相似或更好。此外，还研究了这些同型甾体生物碱的初步构效关系（SARs）。
