中文摘要
老鹳草素 (geraniin) 提取分离自滇产叶下珠植物全草，属多酚类化合物。在省基金资助下，本课题组研究发现，老鹳草素明显抑制维甲酸诱导的大鼠骨质疏松症（OP）。在此基础上，本项目采用去卵巢大鼠模型进一步评价老鹳草素抗OP作用，探讨其抑制破骨细胞（OC）的骨吸收作用。研究老鹳草素对培养的OC II型碳酸酐酶（ CA II）和组织蛋白酶K（CK）蛋白及其mRNA表达的影响。结果表明，老鹳草素呈剂量依赖性明显改善股骨及椎体的骨质疏松病理学变化、改善股骨的骨形态计量学指标，升高骨密度；减少成熟OC及其前体的数目，降低OC形成的陷窝面积、数目及陷窝平均灰度，下调OC中CAII及CK蛋白及其mRNA的表达是其抗OP作用的分子机制。项目实施，证实了老鹳草素的抗OP作用，探索了其细胞分子机制。该项目为将老鹳草素研制成为植物来源和自主创新的抗OP药物提供了临床前药理学研究依据。项目组有3人晋升为高职，1人晋升中职称，2人获硕士学位，1人攻读博士学位。获国家发明专利授权1项，发表论文7篇，获1项云南省社会发展重点项目基金的资助。
英文摘要
Gerannin,a polyphenoid compound, is extracted from Phyllanthus urinaria, a herbal plant native to Yunnan Province.Based on our previously research,which geraniin showed protective effects against tretinoin-induced osteoporosis(OP) in rats, the model of ovary resection of female rats was used to further evaluate its dose-effective relationship of anti-osteoporosis.To elucidate the cellular-molecular biomechanisms of anti-osteoporosis, the effect of geraniin was studied on the protein and mRNA expression of carbonic anhydrase II (CA II) and cathepsin K(CK)in cultured OC.The results showed that geraniin improved the pathological changes of thighbone and vertebral body, as well as the morphometry index of thighbone,increased bone mineral density.Geraniin decreased the total numbers of mature-OC and pre-OC in cultures,and inhibited the total areas, amount and gray scale of OC-induced absorption in bone slices. Geraniin down-regulated the expression of CA II and CK in OC.This project can provide valuable theoretical and experimental evidences for geraniin as a self-innovated and plant-originated anti-osteoporotic drug.Amone our project members, the three were promoted to higher rank,one to medium rank, 2 menbers majored for MD.One authorized patent was obtained, 7 papers pulished,and furthor obtained the project suppo
结题摘要
老鹳草素 (geraniin) 提取分离自滇产叶下珠植物全草，属多酚类化合物。在省基金资助下，本课题组研究发现，老鹳草素明显抑制维甲酸诱导的大鼠骨质疏松症（OP）。在此基础上，本项目采用去卵巢大鼠模型进一步评价老鹳草素抗OP作用，探讨其抑制破骨细胞（OC）的骨吸收作用。研究老鹳草素对培养的OC II型碳酸酐酶（ CA II）和组织蛋白酶K（CK）蛋白及其mRNA表达的影响。结果表明，老鹳草素呈剂量依赖性明显改善股骨及椎体的骨质疏松病理学变化、改善股骨的骨形态计量学指标，升高骨密度；减少成熟OC及其前体的数目，降低OC形成的陷窝面积、数目及陷窝平均灰度，下调OC中CAII及CK蛋白及其mRNA的表达是其抗OP作用的分子机制。项目实施，证实了老鹳草素的抗OP作用，探索了其细胞分子机制。该项目为将老鹳草素研制成为植物来源和自主创新的抗OP药物提供了临床前药理学研究依据。项目组有3人晋升为高职，1人晋升中职称，2人获硕士学位，1人攻读博士学位。获国家发明专利授权1项，发表论文7篇，获1项云南省社会发展重点项目基金的资助。