Kuroda Minpei, Ohshima Takumi, Kan Chihiro, Mimaki Yoshihiro
Nat Prod Commun. 2016 Nov;11(11):1661-1664.
The inhibitory activity of 37 medicinal plant extracts against aldose reductase (AR) activity was evaluated. The most potent AR inhibitory activity was found in the MeOH extract of the leaves of Tussilagofarfara (Compositae). Enzyme assay-guided fractionation of the extract led to the isolation of a new flavonoid glycoside, kaempferol 3-0-[3,4-0-(isopropylidene)-α-L-arabinopyranoside] (1), along with 15 known compounds (2-16), of which 3, 5, 13, 15, and 16 were isolated from T. faifara for the first time. The structures of 1-16 were elucidated based on MS and NMR data. Dicaffeoylquinic acid derivatives (7-12) showed potent AR inhibitory activity with IC(50)values ranging from 0.58 to 5.38 μM, whereas flavonoid glycosides 1, 3, 5, and 6 showed weak inhibitory activity with IC(50) values of 13.9, 15.1, 13.3, and 14.1 μM, respectively.
评估了37种药用植物提取物对醛糖还原酶（AR）活性的抑制作用。发现款冬（菊科）叶的甲醇提取物具有最强的AR抑制活性。对该提取物进行酶活性测定导向的分离，得到一种新的黄酮苷，山柰酚3 - O - [3,4 - O -（亚异丙基）-α - L -阿拉伯吡喃糖苷]（1），以及15种已知化合物（2 - 16），其中3、5、13、15和16首次从款冬中分离得到。基于质谱和核磁共振数据阐明了1 - 16的结构。二咖啡酰奎宁酸衍生物（7 - 12）表现出较强的AR抑制活性，IC（50）值在0.58至5.38μM之间，而黄酮苷1、3、5和6表现出较弱的抑制活性，IC（50）值分别为13.9、15.1、13.3和14.1μM。
