功劳木的化学成分及其体外对P-糖蛋白转运的影响

Chemical constituents from the stem of mahonia bealei(Fort.)carr on p-glycoprotein transport

目的研究功劳木的化学成分,评价其体外对P-糖蛋白转运的影响。方法功劳木用体积分数为70%乙醇提取,得到的浸膏经硅胶干柱色谱分成8份,其中第3～5份和第8份经反复硅胶柱色谱分离得到3个化合物,利用理化性质和波谱数据鉴定了它们的化学结构,并检测3个化合物对耐药细胞株K562/ADM细胞内罗丹明（rhodamine123,Rh123）蓄积的影响。结果显示3个化合物分别为：1-O-（β-D-glucopyranosyl）-（2S,3S,4R,8E）-2-[（2’R）-2’-hydroxytetra cosenoilamino]-8-octadec-ene-1,3,4-triol（1）、erthro-syringoyl glycerol 4-O-β-D-glucoside（2）、葡萄糖（3）。结论化合物1～3为首次从本属植物中分离得到,化合物1和2明显增加耐药细胞株K562/ADM细胞内罗丹明（rhodamine123,Rh123）蓄积量,表现出抑制P-糖蛋白转运功能的活性。

Objective To study the effect of chemical constituents from the stem of Mahonia bealei （Fort.） Carr on P-glycoprotein transport. Methods Mahonia bealei （Fort.） Carr was extracted by 70% alcohol and the extract were separated by dry column chromatography over silica gel into 8 portions. Portions 3-5 and portion 8 were separated and purified by repeated column chromatography on silica gel to get three compounds. Each compound was characterized by spectroscopic and physical data. The effects of three compounds on Rhodamine123 accumulation in K562/ADM cells were detected by high content screening analysis. Results Three compounds have been purified and identified as 1-O-（β-D-glueopyranosyl） -（ 2S, 3S, 4R, 8E）-2- [（2 ＇ R） -2 ＇-hydroxytetracosenoilamino]-8- octadecene 1,3,4-triol（1 ）, erthro-syringoyl glycerol4-O-β D-glucoside （2） and glucose （3） respectively. Conclusion Compounds 1 ～ 3 were obtained for the first time from the genus Mahonia. Compounds 1 and 2 significantly increased accumulation of Rh123 in K562/ADM cells, and showed inhibition of P-glycoprotein transport function.