Zhao Gang, Qin Guo-Wei, Gai Yue, Guo Li-He
Cell Star Bio-Technologies Co., Limited, Shanghai, China.
Chem Pharm Bull (Tokyo). 2010 Jul;58(7):950-2. doi: 10.1248/cpb.58.950.
We previously reported that safflower (Carthamus tinctorius L.) ethyl acetate extract (HE) possessed an inhibitory action on serotonin (5HT) uptake in Chinese hamster ovary (CHO) cells expressing 5HT transporter (SERT) (S6 cells). Here, HE was adopted to go through an activity-guided isolation, and then an ingredient with potent SERT inhibitory action was obtained, which was elucidated as N(1),N(5)-(Z)-N(10)-(E)-tri-p-coumaroylspermidine (CX), a new coumaroylspermidine analog, by using spectroscopic methods including extensive 1D- and 2D-NMR analyses. Preliminary pharmacological study demonstrated that CX was a potent SERT inhibitor.
我们之前报道过，红花（Carthamus tinctorius L.）乙酸乙酯提取物（HE）对表达5-羟色胺转运体（SERT）的中国仓鼠卵巢（CHO）细胞（S6细胞）摄取5-羟色胺（5HT）具有抑制作用。在此，采用HE进行活性导向分离，然后获得了一种具有强效SERT抑制作用的成分，通过包括广泛的一维和二维核磁共振分析在内的光谱方法，将其鉴定为N(1),N(5)-(Z)-N(10)-(E)-三对香豆酰亚精胺（CX），一种新的香豆酰亚精胺类似物。初步药理学研究表明，CX是一种强效SERT抑制剂。
