Lee So Ra, Kim Min-Suk, Kim Sunggun, Hwang Kwang Woo, Park So-Young
Department of Nanomedicine, World Class University, Dankook University, Cheonan, 31116, Korea.
Laboratory of Pharmacognosy, College of Pharmacy, Dankook University, Cheonan, 31116, Korea.
Chem Biodivers. 2017 Nov;14(11). doi: 10.1002/cbdv.201700231. Epub 2017 Nov 3.
The arial parts of Scutellaria barbata D. Don (Lamiaceae) efficiently inhibited NO production in BV2 microglial cells, and the active constituents were further isolated based on activity-guided isolation using silica-gel column chromatography, RP-C18 MPLC and prep-HPLC. As the results, 2 flavonoids including 6-methoxynaringenin (1) and 6-O-methylscutellarein (5), and 6 neo-clerodane diterpenes such as scutebarbatine W (2), scutebatas B (3), scutebarbatine B (4), scutebarbatine A (6), 6-O-nicotinolylscutebarbatine G (7), and scutebarbatine X (8) were isolated. The structures of these compounds were elucidated based on NMR and MS data, and the comparison of literature values. All the compounds except compound 7 inhibited NO production efficiently with IC values of lower than 50 μm. Particularly, compounds 1 and 8 were the most efficient with IC values of 25.8 and 27.4 μm, respectively. This is the first report suggesting the potential of S. barbata on the reduction of neuroinflammation.
半枝莲（唇形科）的地上部分可有效抑制BV2小胶质细胞中一氧化氮（NO）的产生，并通过硅胶柱色谱、RP-C18中压液相色谱和制备型高效液相色谱，基于活性导向分离进一步分离其活性成分。结果分离出2种黄酮类化合物，即6-甲氧基柚皮素（1）和6-O-甲基黄芩素（5），以及6种新克罗烷二萜类化合物，如半枝莲碱W（2）、半枝莲B（3）、半枝莲碱B（4）、半枝莲碱A（6）、6-O-烟酰基半枝莲碱G（7）和半枝莲碱X（8）。这些化合物的结构通过核磁共振（NMR）和质谱（MS）数据以及文献值比较得以阐明。除化合物7外，所有化合物均能有效抑制NO的产生，半数抑制浓度（IC）值低于50 μmol/L。特别是，化合物1和8最为有效，IC值分别为25.8和27.4 μmol/L。这是首次报道半枝莲在减轻神经炎症方面的潜力。
