Im Kyung-Ran, Jeong Tae-Sook, Kwon Byoung-Mog, Baek Nam-In, Kim Sung-Hoon, Kim Dae Keun
College of Pharmacy, Woosuk University, Samrye, Korea.
Arch Pharm Res. 2006 Mar;29(3):191-4. doi: 10.1007/BF02969391.
Twigs from Ilex macropoda were extracted with MeOH, and the concentrated extracts were partitioned with CH2Cl2, EtOAc, n-BuOH, and H2O. Repeated column chromatography of the CH2Cl2 fraction ultimately resulted in the isolation of two compounds, via activity-guided fractionation, using ACAT inhibitory activity measurements. According to the physico-chemical data, the chemical structures of these isolated compounds were identified as lupeol (1) and betulin (2). Compounds 1 and 2 were shown to inhibit the activity of hACAT-1 and hACAT-2 in a dose-dependent manner, and compounds 1 and 2 inhibited hACAT-1 with IC50 values of 48 and 83 microM, respectively.
用甲醇提取大柄冬青的嫩枝，浓缩提取物依次用二氯甲烷、乙酸乙酯、正丁醇和水进行分配。通过活性导向分级分离，利用测定酰基辅酶A胆固醇酰基转移酶（ACAT）抑制活性，对二氯甲烷部分进行反复柱色谱分离，最终分离得到两种化合物。根据物理化学数据，确定这些分离得到的化合物的化学结构分别为羽扇豆醇（1）和桦木醇（2）。化合物1和2均呈剂量依赖性抑制人ACAT-1和人ACAT-2的活性，化合物1和2对人ACAT-1的IC50值分别为48和83微摩尔。
