School of Chinese Medicine, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, People's Republic of China.
Research Division of Pharmacology, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, People's Republic of China.
Fitoterapia. 2014 Apr;94:120-6. doi: 10.1016/j.fitote.2014.01.022. Epub 2014 Feb 4.
Two new diterpenoid alkaloids, Guan-Fu base J (GFJ, 1) and Guan-Fu base N (GFN, 2) along with nineteen known alkaloids (3-21) were isolated from the roots of Aconitum coreanum (Lèvl.) Rapaics, which is the raw material of a new approval anti-arrhythmia drug "Acehytisine Hydrochloride". The structures of isolated compounds were established by means of 1D, 2D NMR spectroscopic and chemical methods. All isolates obtained in the present study were evaluated for their inhibitory effects on blocking the ventricular specific sodium current using a whole-cell patch voltage-clamp technique. Among these 21 compounds, Guan-Fu base S (GFS, 3) showed the strongest inhibitory effect with an IC50 value of 3.48 μM, and only hetisine-type C20 diterpenoid alkaloids showed promising IC50 values for further development.
从具有抗心律失常新药盐酸阿可替尼原料的乌头属植物(Aconitum coreanum (Lèvl.) Rapaics)中分离得到两个新的二萜生物碱，关附甲碱 J (GFJ, 1)和关附甲碱 N (GFN, 2)，以及十九个已知的生物碱 (3-21)。通过 1D、2D NMR 光谱和化学方法确定了分离化合物的结构。采用全细胞膜片钳电压钳技术，评价了本研究中获得的所有分离化合物对阻断心室特异性钠电流的抑制作用。在这 21 种化合物中，关附甲碱 S (GFS, 3)的抑制作用最强，IC50 值为 3.48 μM，只有次乌头型 C20 二萜生物碱具有进一步开发的良好 IC50 值。
