覆盆子抗骨质疏松化学组成及抗骨质疏松活性成分研究

Chemical and Antiosteoporotic Activity Components from Rubus Chingii Hu

目的:探讨覆盆子(Rubus Chingii Hu)的抗骨质疏松化学成份组成及其抗骨质疏松作用。方法:用75%乙醇提取后,再用石油醚,二氯甲烷,正丁醇(水饱和)萃取覆盆子中有效成分,通过核磁及质谱数据分析鉴定成分结构,通过不同化合物对Wistar小鼠成骨和破骨细胞的活性作用,分析不同成分的抗骨质疏松作用。结果:萃取发现覆盆子中包含7种化合物,分别是覆盆子素A(1),覆盆子素B(2),山奈酚(3),槲皮素(4),β-谷甾醇(5),齐墩果酸(6),liballinol(7)。其中覆盆子素B是一种新化合物,研究发现覆盆子素A,覆盆子素B,山奈酚,槲皮素均显示不同程度和特点的抗骨质疏松活性。山奈酚和槲皮素明显的提高碱性磷酸酶(ALP)活性并刺激成骨细胞的活性;而覆盆子素A和覆盆子素B在极低浓度(0.01 ppm)显著的抑制破骨细胞活性以及骨吸收。结论:覆盆子中含有4中抗骨质疏松化合物(覆盆子素A,覆盆子素B,山奈酚,槲皮素),覆盆子素B是发现的一种新化合物。

Objective： To investigate essential components with better antiosteoporotic activity in fruit of the Rubus Chingii Hu. Methods： Extracting dried fruit of Rubus chingii Hu with 75% ethanol extract,the extract was dissolved in H2 O and then was partitioned with sherwood oil,CH2Cl2 and n- butanol. Effective components were identified through checking the NMR and MS data,and antiosteoporotic activity of various components was investigated through the osteoblast and osteoclast from Wistar rats. Results： Totally a new compound rubusin B（ 2） and six known compounds： rubusin A（ 1）,kaempferol（ 3）,quercetin（ 4）,β- sitosterol（ 5）,oleanolic acid（ 6） and liballinol（ 7） were extracted from Rubus Chingii Hu. quercetin and kaempferol significantly increased ALP activity and can stimulate osteoblastic activity,and rubusin A and B strongly inhibit osteoclastic cell and bone resorption even at the concentration of 0. 01 ppm. Conclusions： Four bioactive compounds from Rubus Chingii Hu,containing a new compound（ rubusin B） and three known components（ quercetin,kaempferol and rubusin A） which have antiosteoporotic activity with different characteristics.