啤酒花活性成分黄腐酚抗骨质疏松作用研究

Anti-osteoporotic study on xanthohumol,an active ingredient in Humulus lupulus L.

目的对黄腐酚在动物及成骨细胞水平上的抗骨质疏松作用进行评价。方法采用去卵巢小鼠骨质疏松模型进行体内药效学验证。运用Elisa试剂盒及Micro-CT检测方法,对小鼠血清生化指标及股骨骨密度、骨组织形态学进行评价。同时结合成骨细胞增殖、分化和矿化水平分析,以及骨形成相关蛋白的Western blot检测,对黄腐酚抗骨质疏松作用进行系统评价。结果在体内药效学研究中,黄腐酚可显著提高去卵巢小鼠雌激素水平,降低高骨转换率;改善骨小梁微环境,增强骨密度。在成骨细胞水平上,黄腐酚既可以促进成骨细胞增殖、碱性磷酸酶(ALP)活性以及骨矿化水平,又可以提高骨桥蛋白(OPN)、骨涎蛋白(BSP)和骨形成蛋白(BMP-2)的表达。结论本研究首次明确了黄腐酚具有抗骨质疏松作用,为开发治疗骨质疏松的药物提供新的资源。

Objective To evaluate the anti-osteoporotic effect of xanthohumol（XN）in animal and osteoblast.MethodsThe anti-osteoporotic study on XN was performed with ovariectomized mice model.Serum biochemical indexes,bone mineral density（BMD）and bone histomorphology were measured using Elisa kits and Micro-CT analysis.In vitro test,the effect of XN on osteoblastic proliferation,differentiation and mineralization were assayed.The expression of protein related to bone formation was measured by Western blot analysis.Results In vivo experiments,XN significantly increased the estrogen level,reduced the high bone turnover rate,improved the microenvironment and BMD in ovariectomized mice.In vitro experiments,XN protected bone loss not only by promoting osteoblastic proliferation,ALP activity and bone mineralization,but also through increasing the expression of osteopontin（OPN）,bone sialoprotein（BSP）and bone morphogenetic protein-2（BMP-2）.Conclusion This is the first report to confirm that XN has anti-osteoporotic effect,which provides a new approach for the clinical treatment of osteoporosis.